NSCLCPhase 1FRAMENCT03875820
Phase I Trial of Defactinib and VS-6766.
A Phase 1 study testing VS-6766 and Defactinib in people with NSCLC and Low Grade Serous Ovarian Cancer, run by Institute of Cancer Research, United Kingdom at 5 sites in United Kingdom.
Trial summary
This is a multi-centre, investigator-initiated, dose escalation, Phase I trial of the combination of the FAK inhibitor, Defactinib (VS-6063), and the dual RAF/MEK inhibitor, VS-6766 (RO5126766) in patients with advanced solid tumours. VS-6766 (RO5126766) is the same compound as CH5126766. Read more about this study
- Who is it for?
- Ages 18 years and older
- Conditions the study is for
- NSCLC, Low Grade Serous Ovarian Cancer, Endometrioid Carcinoma
- What is being tested?
- VS-6766 and Defactinib
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 87 participants
- Where
- 5 sitesUnited Kingdom
- Study dates
- 12 Dec 2017to 31 Oct 2026
- Phase
- Phase 1
- Are there results?
- Not yet: the study is under way
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 years and older
- All sexes
- No healthy volunteers
- Adult, Older adult
Who may be able to join
- Dose escalation:
- Histologically or cytologically proven solid tumours, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient enriching for patients with RAS mutant solid tumours.
- Dose expansion:
- Histologically or cytologically proven advanced non-small-cell lung cancer (NSCLC) with a documented KRAS mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (20 patients).
- OR Histologically or cytologically proven advanced low grade serous ovarian cancer (LGSOC), refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (20 patients).
- OR Histologically or cytologically proven advanced colorectal cancer (CRC) with a documented RAS mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (10 patients).
Show all 26Show fewer
- OR Histologically or cytologically proven RAS mutant solid tumours, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient. Patient must have biopsiable disease, be willing and has consented to undergo biopsies at three time-points (6 patients).
- OR Histologically or cytologically proven advanced pancreatic cancer or metastatic pancreatic cancer, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (10 patients).
- OR Endometroid subtype of gynaecological cancers (ovarian, endometrial, endometriosis related) with a documented RAS or RAF mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (10 patients).
- OR Histologically or cytologically proven advanced non-small-cell lung cancer (NSCLC) with a documented KRAS G12V specific mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (10 patients).
- Predicted life expectancy of at least 12 weeks
- World Health Organisation (WHO) performance status of 0 or 1 (Appendix 1)
- Haematological and biochemical indices within the ranges shown below. These measurements must be performed within one week (Day -7 to Day 1) before the patient goes in the trial.
- Haemoglobin (Hb) ≥ 9.0 g/dL Absolute neutrophil count (ANC) ≥ 1.5 x 109/L Platelet count ≥ 100 x 109/L Serum bilirubin ≤ 1.5 x upper limit of normal (ULN) Alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)
- ≤ 2.5 x (ULN) unless raised due to tumour in which case up to 5 x ULN is permissible
- Either:
- Calculated creatinine clearance ≥ 50 mL/min (uncorrected value)
- Or:
- Serum creatinine ≤ 1.5 x ULN
- Men and women aged 18 years or over.
- Written (signed and dated) informed consent and be capable of co-operating with treatment and follow-up.
- Absence of any psychological, familial, sociological or geographical condition potentially hampering compliance with the study protocol and follow-up schedule.
- Dose escalation: Measurable disease according to RECIST 1.1 or evaluable disease. All radiology studies must be performed within 28 days prior to registration.
- Dose expansion: Measurable disease according to RECIST 1.1, all radiology studies must be performed within 28 days prior to registration.
- Corrected QT interval (QTc) < 470 ms (as calculated by the Fridericia correction formula, averaged over 3 ECGs).
- Agrees to the use of archival paraffin embedded tissue and has archival tumour tissue available.
Who cannot join
- Radiotherapy (except for palliative reasons), endocrine therapy, biological therapy, immunotherapy or chemotherapy during the previous four weeks (six weeks for nitrosoureas, Mitomycin-C) before treatment.
- Ongoing toxic manifestations of previous treatments. Exceptions to this are alopecia or certain Grade 1 toxicities, which in the opinion of the Investigator and the DDU should not exclude the patient.
- Known untreated or active central nervous system (CNS) metastases (progressing or requiring corticosteroids for symptomatic control). Patients with a history of treated CNS metastases are eligible, provided they meet all of the following criteria:
- Evaluable or measurable disease outside the CNS is present.
- Radiographic demonstration of improvement upon the completion of CNS-directed therapy and no evidence of interim progression between the completion of CNS-directed therapy and the baseline disease assessment for at least 28 days.
- Ability to become pregnant (or already pregnant or lactating). However, those female patients who have a negative serum or urine pregnancy test before enrolment and agree to use two medically approved forms of contraception (oral, injected or implanted hormonal contraception and condom, have an intra-uterine device and condom, diaphragm with spermicidal gel and condom) from time of consent, during the trial and for six months afterwards are considered eligible.
Show all 24Show fewer
- Male patients with partners of child-bearing potential (unless they agree to take measures not to father children by using one form of medically approved contraception [condom plus spermicide] during the trial and for six months afterwards). Men with pregnant or lactating partners should be advised to use barrier method contraception (for example, condom plus spermicidal gel) to prevent exposure to the foetus or neonate.
- Major surgery within 4 weeks prior to entry to the study (excluding placement of vascular access), or minor surgery within 2 weeks of entry into the study and from which the patient has not yet recovered.
- Treatment with warfarin. Patients on warfarin for DVT/PE can be converted to LMWH.
- Known history of Gilbert's Syndrome.
- Acute or chronic pancreatitis.
- At high medical risk because of non-malignant systemic disease including active uncontrolled infection.
- Known to be serologically positive for hepatitis B, hepatitis C or human immunodeficiency virus (HIV).
- Patients with the inability to swallow oral medications or impaired gastrointestinal absorption due to gastrectomy or active inflammatory bowel disease.
- Concurrent ocular disorders:
- Patients with history of glaucoma, history of retinal vein occlusion (RVO), predisposing factors for RVO, including uncontrolled hypertension, uncontrolled diabetes
- Patient with history of retinal pathology or evidence of visible retinal pathology that is considered a risk factor for RVO, intraocular pressure > 21mm Hg as measured by tonometry, or other significant ocular pathology, such as anatomical abnormalities that increase the risk for RVO.
- Patients with a history of corneal erosion (instability of corneal epithelium), corneal degeneration, active or recurrent keratitis, and other forms of serious ocular surface inflammatory conditions.
- Concurrent congestive heart failure, prior history of class III/ IV cardiac disease (New York Heart Association [NYHA] - refer to Appendix 4), myocardial infarction within the last 6 months, unstable arrhythmias, unstable angina or severe obstructive pulmonary disease.
- Patients exposed to strong CYP3A4 and strong CYP2C9 inhibitors within 7 days prior to the first dose.
- N.B. Because the lists of these agents are constantly changing, it is important to regularly consult a frequently-updated list such as http://medicine.iupui.edu/clinpharm/ddis/table.aspx; medical reference texts such as the Physicians' Desk Reference may also provide this information.
- Is a participant or plans to participate in another interventional clinical trial, whilst taking part in this Phase I study of VS-6766 in combination with Defactinib. Participation in an observational trial would be acceptable.
- Symptoms of COVID-19 and/or documented current COVID-19 infection (the patient can be reassessed for eligibility following a full recovery and negative COVID-19 test).
- Any other condition which in the Investigator's opinion would not make the patient a good candidate for the clinical trial.
Trial locations and contacts
5 sites in 1 country.
5 sites in 1 country
United Kingdom5 sites
The Royal Marsden NHS Foundation Trust - Gynecology Unit
London, SW3 6JJ
The Christie NHS Foundation Trust
Manchester, Greater Manchester, M20 4BX
The Newcastle Upon Tyne Hospitals NHS Foundation Trust - Freeman Hospital
Newcastle, NE7 7DN
The Royal Marsden NHS Foundation Trust
Sutton, Surrey, SM2 5PT
The Royal Marsden NHS Foundation Trust - Gynecology Unit
Sutton, SM2 5PT
About this study
Official title: FRAME: A Phase I Trial of the Combination of Defactinib (VS-6063) (FAK Inhibitor) and VS-6766 (RO5126766) (CH5126776) (a Dual RAF/MEK Inhibitor) in Patients With Advanced Solid Tumours
This is a multi-centre, investigator-initiated, dose escalation, Phase I trial of the combination of the FAK inhibitor, Defactinib (VS-6063), and the dual RAF/MEK inhibitor, VS-6766 (RO5126766) in patients with advanced solid tumours. VS-6766 (RO5126766) is the same compound as CH5126766.
There are two parts to this study, the dose escalation phase and the dose expansion phase. In the dose escalation phase, cohorts of 3 to 6 patients will be enrolled to determine the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D). This will be followed by a dose expansion phase to further characterise the safety and tolerability and to assess the pharmacodynamic activity of the combination.
Read the detailed description
This is a multi-centre, investigator-initiated, dose escalation, Phase I trial of the combination of the FAK inhibitor, Defactinib, and the dual RAF/MEK inhibitor, VS-6766 in patients with advanced solid tumours.
There are two parts to this study, the dose escalation phase and the dose expansion phase. In the dose escalation phase, cohorts of 3 to 6 patients were enrolled to determine the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D). Up to 24 patients with solid tumours were treated in the dose escalation phase of this study.
The dose escalation phase is now closed to recruitment.
This will be followed by a dose expansion phase of 86 patients to further characterise the safety and tolerability and to assess the pharmacodynamic activity of the combination.
The dose expansion phase is made up of 7 cohorts:
- 20 patients with KRAS mutant non-small-cell lung cancer (NSCLC);
- 7 patients with solid tumours (enriched for those with RAS mutations) willing to undergo biopsies at three time points throughout the study;
- 20 patients with low grade serous ovarian cancer (LGSOC);
- 10 patients with colorectal cancer (CRC);
- 10 patients with KRAS G12V mutant NSCLC;
- 10 patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis related) and
- 10 patients with pancreatic cancer.
The following cohorts are still open to recruitment:
- Patients with low grade serous ovarian cancer (LGSOC);
- Patients with KRAS G12V mutant NSCLC;
- Patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis-related) and
- Patients with pancreatic cancer.
Patients will take the two investigational medicinal products (IMPs) as follows:
VS-6766 will be administered orally twice a week on Monday/Thursday or Tuesday/Friday at least one hour prior or two hours after a meal. The starting dose of VS-6766 will be 3.2mg once a day, twice a week and can be escalated to a maximum of 4mg once a day, twice a week.
Defactinib will be administered orally twice a day immediately after a meal. The starting dose of Defactinib will be 200mg twice daily and can be escalated to a maximum of 400mg twice daily.
A cycle length is 4 weeks (28 days). Combination dosing (VS-6766 and Defactinib) will commence on Cycle 1 Day 1 for 3 weeks followed by one week without either drug in week 4 (i.e. 3 weeks on, 1 week off).
For patients consenting to optional biopsies, a run-in dose of VS-6766 will be administered on a single day anywhere between Days -7 to Day -3 in order to facilitate pharmacodynamic (PD) biomarker analysis. Therefore, for patients undergoing biopsies the first cycle will be 5 weeks long and subsequent cycles will consist of 4 weeks.
If this schedule is not tolerated, alternative schedules may be explored following discussion by the Safety Review Committee.
- Being tested
- VS-6766, Defactinib
- Keywords
- KRAS G12V, RAS, RAF
- Medical subject headings
- Carcinoma, Endometrioid, Pancreatic Neoplasms
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
VS-6766Drug
Also called RO5126766, CH5126766
VS-6766 will be supplied as 0.8mg hypromellose (HPMC) capsules for oral administration. The capsule fill consists of VS-6766 and the inactive ingredients mannitol and magnesium stearate.
VS-6766 will be administered on a twice weekly (Monday and Thursday or Tuesday and Friday) schedule for 3 weeks followed by 1 week off in every 4 week cycle, under fasting conditions (approximately 1 hour prior or 2 hours after a meal). The starting dose, based on the previous Phase I trial will be 3.2 mg given orally as a single daily dose. This can be escalated to a maximum of 4mg (as per dose escalation rules in the protocol).
DefactinibDrug
Also called VS-6063
Defactinib is formulated as a white to off-white oval tablet for oral administration and supplied in single unit dose strength of 200 mg in 120 cc (HDPE) bottles. In addition to Defactinib, formulation components include microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, and magnesium stearate.
Patients will receive Defactinib orally immediately after a meal twice daily (approximately every 12 hours) for 3 weeks followed by 1 week off in every 4 week cycle. The starting dose will be 200mg. This can be escalated to a maximum of 400mg (as per dose escalation rules in the protocol).
| Study group | Role | What they receive |
|---|---|---|
| Dose Escalation Phase | Experimental | Escalating doses of VS-6766 (RO5126766) and Defactinib (VS-6063) were evaluated in patients with advanced solid tumours to establish the recommended phase II dose. Dose escalation followed a 3+3 design with a maximum of four patient cohorts.
This arm is now complete. Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion KRAS mutant NSCLC Cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with KRAS mutant NSCLC (20 patients).
This arm is now complete. Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion biopsy cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients advanced RAS mutant solid tumours with biopsiable disease (6 patients).
This arm is now complete. Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion LGSOC cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with LGSOC (20 patients). Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion CRC cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with CRC (10 patients).
This arm is now complete. Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion KRAS G12V mutant NSCLC cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with KRAS G12V mutant NSCLC (10 patients). Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion RAS/RAF mutant endometrioid cancer cohort | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis-related) (10 patients). Receives: Drug: VS-6766; Drug: Defactinib |
| Dose Expansion pancreatic cancer | Experimental | The dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with pancreatic cancer (10 patients). Receives: Drug: VS-6766; Drug: Defactinib |
What is being measured
The primary outcome is the main question the study is designed to answer.
To establish a dose for Phase II evaluation from the maximum tolerated dose of the combination of VS-6766 and Defactinib.
To determine the maximum dose at which no more than 1 of 6 patients at the same dose level experience a drug related toxicity (DLT) as specified in the protocol.
Measured: 12 months
Measure Adverse Events according to CTCAE v4.0.
To assess the safety and toxicity profile of VS-6766 and Defactinib. To determine causality and grading severity of each adverse event by National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0.
Measured: 6 months
Secondary outcomes (3)
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Determination of the PK parameter Cmax of VS-6766 and Defactinib when dosed together.
Measured: 12 months
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Determination of the PK parameter terminal half-life of VS-6766 and Defactinib when dosed together.
Measured: 12 months
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Determination of the PK parameter area under the curve of VS-6766 and Defactinib when dosed together.
Measured: 12 months
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted15 Mar 2019
- Study start12 Dec 2017
- Primary completion30 Apr 2023
- Study completion31 Oct 2026 (estimated)
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (2)Papers the sponsor has linked to this study.
- Other trials for NSCLCStudies of the same condition, open and under way.
- More trials run by Institute of Cancer Research, United KingdomThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Health services research
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Model description
- The dose escalation phase will enrol patients with advanced RAS mutant solid tumours. In the dose expansion phase, patients are assigned to one of the following cohorts based on their diagnosis: * KRAS mutant NSCLC cohort * LGSOC cohort * RAS mutant CRC cohort * Advanced RAS mutant solid tumour cohort - patients in this cohort must have biopsiable disease, be willing and consent to undergo biopsies at three time-points. * KRAS G12V mutant NSCLC cohort * RAS/RAF mutant endometrioid cohort * Pancreatic cohort
- Masking
- None (open label)
- Enrolment
- 87 participants (actual)
Sponsor and investigators
- Lead sponsor
- Institute of Cancer Research, United Kingdom
- Sponsor type
- University, hospital or other
- Collaborators
- Verastem, Inc.
- Responsible party
- Sponsor
- Investigators
- Udai Banerji, FRCP, PhD, Principal investigator, Institute of Cancer Research, United Kingdom
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT03875820
- Sponsor's protocol ID
- CCR4642
- Other IDs
- 2017-001035-39, 2017
- Acronym
- FRAME
- Status last verified
- Mar 2026
- First submitted
- 15 Nov 2018
- Last updated
- 10 Mar 2026
- Results posted
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No
Publications
Banerjee S, Krebs MG, Greystoke A, Garces AI, Perez VS, Terbuch A, Shinde R, Caldwell R, Grochot R, Rouhifard M, Ruddle R, Gurel B, Swales K, Tunariu N, Prout T, Parmar M, Symeonides S, Rekowski J, Yap C, Sharp A, Paschalis A, Lopez J, Minchom A, de Bono JS, Banerji U. Defactinib with avutometinib in patients with solid tumors: the phase 1 FRAME trial. Nat Med. 2025 Sep;31(9):3074-3080. doi: 10.1038/s41591-025-03763-y. Epub 2025 Jun 27.
PubMed 40579546Fard D, Giraudo E, Tamagnone L. Mind the (guidance) signals! Translational relevance of semaphorins, plexins, and neuropilins in pancreatic cancer. Trends Mol Med. 2023 Oct;29(10):817-829. doi: 10.1016/j.molmed.2023.07.009. Epub 2023 Aug 17.
PubMed 37598000
Study at a glance
From the registry record, last updated by the sponsor on 10 Mar 2026. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- FRAME: A Phase I Trial of the Combination of Defactinib (VS-6063) (FAK Inhibitor) and VS-6766 (RO5126766) (CH5126776) (a Dual RAF/MEK Inhibitor) in Patients With Advanced Solid Tumours
- ClinicalTrials.gov ID
- NCT03875820
- Acronym / sponsor ID
- FRAME / CCR4642
- Keywords
- KRAS G12V, RAS, RAF
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Active, not recruiting
- Enrolment
- 87 participants (actual)
- Lead sponsor
- Institute of Cancer Research, United KingdomUniversity, hospital or other
- Collaborators
- Verastem, Inc.
- Study start
- 12 Dec 2017 (actual)
- Primary completion
- 30 Apr 2023 (actual)
- Study completion
- 31 Oct 2026 (estimated)
- First posted
- 15 Mar 2019 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is a multi-centre, investigator-initiated, dose escalation, Phase I trial of the combination of the FAK inhibitor, Defactinib (VS-6063), and the dual RAF/MEK inhibitor, VS-6766 (RO5126766) in patients with advanced solid tumours. VS-6766 (RO5126766) is the same compound as CH5126766.
There are two parts to this study, the dose escalation phase and the dose expansion phase. In the dose escalation phase, cohorts of 3 to 6 patients will be enrolled to determine the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D). This will be followed by a dose expansion phase to further characterise the safety and tolerability and to assess the pharmacodynamic activity of the combination.
Detailed description
This is a multi-centre, investigator-initiated, dose escalation, Phase I trial of the combination of the FAK inhibitor, Defactinib, and the dual RAF/MEK inhibitor, VS-6766 in patients with advanced solid tumours.
There are two parts to this study, the dose escalation phase and the dose expansion phase. In the dose escalation phase, cohorts of 3 to 6 patients were enrolled to determine the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D). Up to 24 patients with solid tumours were treated in the dose escalation phase of this study.
The dose escalation phase is now closed to recruitment.
This will be followed by a dose expansion phase of 86 patients to further characterise the safety and tolerability and to assess the pharmacodynamic activity of the combination.
The dose expansion phase is made up of 7 cohorts:
- 20 patients with KRAS mutant non-small-cell lung cancer (NSCLC);
- 7 patients with solid tumours (enriched for those with RAS mutations) willing to undergo biopsies at three time points throughout the study;
- 20 patients with low grade serous ovarian cancer (LGSOC);
- 10 patients with colorectal cancer (CRC);
- 10 patients with KRAS G12V mutant NSCLC;
- 10 patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis related) and
- 10 patients with pancreatic cancer.
The following cohorts are still open to recruitment:
- Patients with low grade serous ovarian cancer (LGSOC);
- Patients with KRAS G12V mutant NSCLC;
- Patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis-related) and
- Patients with pancreatic cancer.
Patients will take the two investigational medicinal products (IMPs) as follows:
VS-6766 will be administered orally twice a week on Monday/Thursday or Tuesday/Friday at least one hour prior or two hours after a meal. The starting dose of VS-6766 will be 3.2mg once a day, twice a week and can be escalated to a maximum of 4mg once a day, twice a week.
Defactinib will be administered orally twice a day immediately after a meal. The starting dose of Defactinib will be 200mg twice daily and can be escalated to a maximum of 400mg twice daily.
A cycle length is 4 weeks (28 days). Combination dosing (VS-6766 and Defactinib) will commence on Cycle 1 Day 1 for 3 weeks followed by one week without either drug in week 4 (i.e. 3 weeks on, 1 week off).
For patients consenting to optional biopsies, a run-in dose of VS-6766 will be administered on a single day anywhere between Days -7 to Day -3 in order to facilitate pharmacodynamic (PD) biomarker analysis. Therefore, for patients undergoing biopsies the first cycle will be 5 weeks long and subsequent cycles will consist of 4 weeks.
If this schedule is not tolerated, alternative schedules may be explored following discussion by the Safety Review Committee.
Study design
- Primary purpose
- Health services research
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Number of arms
- 8
- Model description
- The dose escalation phase will enrol patients with advanced RAS mutant solid tumours. In the dose expansion phase, patients are assigned to one of the following cohorts based on their diagnosis: * KRAS mutant NSCLC cohort * LGSOC cohort * RAS mutant CRC cohort * Advanced RAS mutant solid tumour cohort - patients in this cohort must have biopsiable disease, be willing and consent to undergo biopsies at three time-points. * KRAS G12V mutant NSCLC cohort * RAS/RAF mutant endometrioid cohort * Pancreatic cohort
| Arm | Type | Receives |
|---|---|---|
| Dose Escalation Phase | Experimental | Drug: VS-6766, Drug: DefactinibEscalating doses of VS-6766 (RO5126766) and Defactinib (VS-6063) were evaluated in patients with advanced solid tumours to establish the recommended phase II dose. Dose escalation followed a 3+3 design with a maximum of four patient cohorts. This arm is now complete. |
| Dose Expansion KRAS mutant NSCLC Cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with KRAS mutant NSCLC (20 patients). This arm is now complete. |
| Dose Expansion biopsy cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients advanced RAS mutant solid tumours with biopsiable disease (6 patients). This arm is now complete. |
| Dose Expansion LGSOC cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with LGSOC (20 patients). |
| Dose Expansion CRC cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with CRC (10 patients). This arm is now complete. |
| Dose Expansion KRAS G12V mutant NSCLC cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with KRAS G12V mutant NSCLC (10 patients). |
| Dose Expansion RAS/RAF mutant endometrioid cancer cohort | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with RAS/RAF mutant endometrioid subtype of gynaecological cancers (ovarian, endometrial, endometriosis-related) (10 patients). |
| Dose Expansion pancreatic cancer | Experimental | Drug: VS-6766, Drug: DefactinibThe dose expansion phase will evaluate the recommended phase II dose of the combination of VS-6766 (RO5126766) and Defactinib (VS-6063), as decided in the dose escalation phase in patients with pancreatic cancer (10 patients). |
Who may qualify
- Ages
- 18 years and older
- Sex
- All
- Healthy volunteers
- Not accepted
- Age groups
- Adult, Older adult
Key inclusion criteria (26 listed)
- Dose escalation:
- Histologically or cytologically proven solid tumours, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient enriching for patients with RAS mutant solid tumours.
- Histologically or cytologically proven advanced non-small-cell lung cancer (NSCLC) with a documented KRAS mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (20 patients).
- OR Histologically or cytologically proven advanced low grade serous ovarian cancer (LGSOC), refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (20 patients).
- OR Histologically or cytologically proven advanced colorectal cancer (CRC) with a documented RAS mutation, refractory to conventional treatment, or for which no conventional therapy exists or is declined by the patient (10 patients).
Key exclusion criteria (24 listed)
- Radiotherapy (except for palliative reasons), endocrine therapy, biological therapy, immunotherapy or chemotherapy during the previous four weeks (six weeks for nitrosoureas, Mitomycin-C) before treatment.
- Ongoing toxic manifestations of previous treatments. Exceptions to this are alopecia or certain Grade 1 toxicities, which in the opinion of the Investigator and the DDU should not exclude the patient.
- Known untreated or active central nervous system (CNS) metastases (progressing or requiring corticosteroids for symptomatic control). Patients with a history of treated CNS metastases are eligible, provided they meet all of the following criteria:
- Ability to become pregnant (or already pregnant or lactating). However, those female patients who have a negative serum or urine pregnancy test before enrolment and agree to use two medically approved forms of contraception (oral, injected or implanted hormonal contraception and condom, have an intra-uterine device and condom, diaphragm with spermicidal gel and condom) from time of consent, during the trial and for six months afterwards are considered eligible.
- Male patients with partners of child-bearing potential (unless they agree to take measures not to father children by using one form of medically approved contraception [condom plus spermicide] during the trial and for six months afterwards). Men with pregnant or lactating partners should be advised to use barrier method contraception (for example, condom plus spermicidal gel) to prevent exposure to the foetus or neonate.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| VS-6766Also: RO5126766, CH5126766VS-6766 will be supplied as 0.8mg hypromellose (HPMC) capsules for oral administration. The capsule fill consists of VS-6766 and the inactive ingredients mannitol and magnesium stearate. VS-6766 will be administered on a twice weekly (Monday and Thursday or Tuesday and Friday) schedule for 3 weeks followed by 1 week off in every 4 week cycle, under fasting conditions (approximately 1 hour prior or 2 hours after a meal). The starting dose, based on the previous Phase I trial will be 3.2 mg given orally as a single daily dose. This can be escalated to a maximum of 4mg (as per dose escalation rules in the protocol). | Drug | Dose Escalation Phase, Dose Expansion CRC cohort, Dose Expansion KRAS G12V mutant NSCLC cohort, Dose Expansion KRAS mutant NSCLC Cohort, Dose Expansion LGSOC cohort, Dose Expansion RAS/RAF mutant endometrioid cancer cohort, Dose Expansion biopsy cohort, Dose Expansion pancreatic cancer |
| DefactinibAlso: VS-6063Defactinib is formulated as a white to off-white oval tablet for oral administration and supplied in single unit dose strength of 200 mg in 120 cc (HDPE) bottles. In addition to Defactinib, formulation components include microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, and magnesium stearate. Patients will receive Defactinib orally immediately after a meal twice daily (approximately every 12 hours) for 3 weeks followed by 1 week off in every 4 week cycle. The starting dose will be 200mg. This can be escalated to a maximum of 400mg (as per dose escalation rules in the protocol). | Drug | Dose Escalation Phase, Dose Expansion CRC cohort, Dose Expansion KRAS G12V mutant NSCLC cohort, Dose Expansion KRAS mutant NSCLC Cohort, Dose Expansion LGSOC cohort, Dose Expansion RAS/RAF mutant endometrioid cancer cohort, Dose Expansion biopsy cohort, Dose Expansion pancreatic cancer |
Primary outcome
To establish a dose for Phase II evaluation from the maximum tolerated dose of the combination of VS-6766 and Defactinib.
Time frame: 12 months
To determine the maximum dose at which no more than 1 of 6 patients at the same dose level experience a drug related toxicity (DLT) as specified in the protocol.
Measure Adverse Events according to CTCAE v4.0.
Time frame: 6 months
To assess the safety and toxicity profile of VS-6766 and Defactinib. To determine causality and grading severity of each adverse event by National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0.
3 secondary outcomes
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Time frame: 12 months
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Time frame: 12 months
To characterise the pharmacokinetic profile of VS-6766 in combination with Defactinib.
Time frame: 12 months
Results and safety
This study is still under way. Results are not available in the source record yet.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 10 Mar 2026.
- Derived from this study: PubMed 40579546Banerjee S, Krebs MG, Greystoke A, Garces AI, Perez VS, Terbuch A, Shinde R, Caldwell R, Grochot R, Rouhifard M, Ruddle R, Gurel B, Swales K, Tunariu N, Prout T, Parmar M, Symeonides S, Rekowski J, Yap C, Sharp A, Paschalis A, Lopez J, Minchom A, de Bono JS, Banerji U. Defactinib with avutometinib in patients with solid tumors: the phase 1 FRAME trial. Nat Med. 2025 Sep;31(9):3074-3080. doi: 10.1038/s41591-025-03763-y. Epub 2025 Jun 27.
- Derived from this study: PubMed 37598000Fard D, Giraudo E, Tamagnone L. Mind the (guidance) signals! Translational relevance of semaphorins, plexins, and neuropilins in pancreatic cancer. Trends Mol Med. 2023 Oct;29(10):817-829. doi: 10.1016/j.molmed.2023.07.009. Epub 2023 Aug 17.
- Individual participant dataSharing planned: No
Related trials for NSCLC
RecruitingPhase 1/2
Study of INBRX-106 and INBRX-106 in Combination With Pembrolizumab (Keytruda®) in Subjects With Locally Advanced or Metastatic Solid Tumors (Hexavalent OX40 Agonist)
Solid Tumor, Non-Small Cell Lung Cancer
RecruitingObservational study
A Prospective ,Multicenter ,Non-interventional ,Real-world Study Observing Changes in Molecular Markers Osimertinib Targeted Therapy in EGFRm NSCLC
Non Small Cell Lung Cancer
RecruitingPhase 3
A Study Evaluating Sotorasib Platinum Doublet Combination Versus Pembrolizumab Platinum Doublet Combination as a Front-Line Therapy in Participants With Stage IV or Advanced Stage IIIB/C Nonsquamous Non-Small Cell Lung Cancers (CodeBreaK 202)
Non-Small Cell Lung Cancer (NSCLC)
Active, not recruitingPhase 2
Datopotamab Deruxtecan (Dato-DXd, DS-1062a) in Advanced and/or Unresectable Non-Small Cell Lung Cancer
Metastatic Lung Cancer, Advanced Non Small Cell Lung Cancer
Not yet recruitingPhase 1/2
STAR0602 With Nivolumab in Non Small Cell Lung Cancer and in Metastatic Castrate-Resistant Prostate Cancer, and STAR0602 Alone in Thymic Carcinoma
NSCLC, Non-Small Cell Lung Cancer
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Udai Banerji, FRCP, PhD principal investigator
Institute of Cancer Research, United Kingdom
5 sites in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing VS-6766 and Defactinib in people with NSCLC and Low Grade Serous Ovarian Cancer, run by Institute of Cancer Research, United Kingdom at 5 sites in United Kingdom.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 26 inclusion and 24 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: under way, not looking for participants, as of the sponsor's last update on 10 Mar 2026. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 5 sites in United Kingdom. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
This study is still under way. Results are not available in the source record yet.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
To establish a dose for Phase II evaluation from the maximum tolerated dose of the combination of VS-6766 and Defactinib. (time frame: 12 months). The study lists 2 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT03875820, which also lists 2 linked publications.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 10 Mar 2026.