Locally Advanced or Metastatic ER+ HER2- Breast CancerPhase 2KAT6NCT04606446
Study of PF-07248144 in Advanced or Metastatic Solid Tumors
A Phase 2 study testing PF-07248144, Fulvestrant and Letrozole in people with Locally Advanced or Metastatic ER+ HER2- Breast Cancer and Locally Advanced or Metastatic Castration-resistant Prostate Cancer, run by Pfizer at 43 sites in 5 countries.
Trial summary
This is an open-label, multi center study to evaluate safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of PF-07248144 and early signs of clinical efficacy of PF-07248144 as a single agent and in combination with other agents Read more about this study
- Who is it for?
- Ages 18 years and older
- Conditions the study is for
- Locally Advanced or Metastatic ER+ HER2- Breast Cancer, Locally Advanced or Metastatic Castration-resistant Prostate Cancer, Locally Advanced or Metastatic Non-small Cell Lung Cancer
- What is being tested?
- PF-07248144, Fulvestrant and Letrozole
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 320 participants
- Where
- 43 sitesin 5 countries
- Study dates
- 16 Nov 2020to 27 Aug 2029
- Phase
- Phase 2
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
- Disease Characteristics - Breast, Prostate, and Lung Cancer
- Part 1A (Monotherapy Dose Escalation) Histological or cytological diagnosis of locally advanced or metastatic ER+HER2- breast cancer, CRPC, or NSCLC that is intolerant or resistant to standard therapy or for which no standard therapy is available.
- Part 1B, Part 1C, Part 1D and Part 1E (Combination Dose Escalation) Histological or cytological diagnosis of locally advanced or metastatic ER+HER2- breast cancer. Participants must have progressed after at least 1 prior line of treatment with an endocrine therapy and CDK4/6 inhibitor in the advanced or metastatic setting.
- Part 2A (ER+HER2- breast cancer 2L+, monotherapy) Histological or cytological diagnosis of locally advanced or metastatic ER+HER2- breast cancer. Participants must have progressed after at least 1 prior line of CDK4/6 inhibitor and 1 line of endocrine therapy.
- Part 2B (ER+HER2- breast cancer 2-4L, combination with fulvestrant) Histological or cytological diagnosis of advanced or metastatic ER+HER2- breast cancer. Participants must have progressive disease after at least 1 prior line of a CDK4/6 inhibitor and at least 1 prior line of endocrine therapy.. Participants must not have received more than 3 prior lines of systemic therapies including up to 1 line of cytotoxic chemotherapy for visceral disease in advanced or metastatic setting; Participants may have but are not required to have prior treatment with fulvestrant.
- Part 2D (ER+HER2- breast cancer 2-4L, combination with PF-07220060 (CDK4i) and fulvestrant):
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- Histological or cytological diagnosis of advanced or metastatic ER+HER2- breast cancer. Participants must have progressive disease after at least 1 prior line of a CDK4/6 inhibitor and at least 1 prior line of endocrine therapy.
- Participants must have not received more than 3 lines of systemic therapies including up to 1 line of cytotoxic chemotherapy for visceral disease in advanced or metastatic setting; Participants may have but are not required to have prior treatment with fulvestrant.
- Part 2E (ER+HER2- breast cancer 2-4L, combination with vepdegestrant): Histological or cytological diagnosis of advanced or metastatic ER+HER2- breast cancer. Participants must have progressive disease after at least 1 prior line of a CDK4/6 inhibitor and at least 1 prior line of endocrine therapy; Participants must have not received more than 3 lines of systemic therapies including up to 1 line of cytotoxic chemotherapy for visceral disease in advanced or metastatic setting; Participants may have received fulvestrant
- Participants with ER+HER2- advanced or metastatic breast cancer must have documentation of ER-positive tumor (≥1% positive stained cells) based on most recent tumor biopsy utilizing an assay consistent with local standards.
- Participants with ER+HER2- advanced or metastatic breast cancer must have documentation of HER2-negative tumor: HER2-negative tumor is determined as immunohistochemistry score 0/1+ or negative by in situ hybridization (FISH/CISH/SISH/DISH) defined as a HER2/CEP17 ratio <2 or for single probe assessment a HER2 copy number <4.
- Female participants with ER+HER2- advanced or metastatic breast cancer considered to be of childbearing potential (or have tubal ligations only) must be willing to undergo medically induced menopause by treatment with the approved LHRH agonist such as goserelin, leuprolide or equivalent agents to induce chemical menopause.
- Female participants with ER+HER2- advanced or metastatic breast cancer of nonchildbearing potential must meet at least 1 criteria of achieving postmenopausal status.
- Participants must have at least 1 measurable lesion as defined by RECIST version 1.1 that has not been previously irradiated.
- Eastern Cooperative Oncology Group (ECOG) Performance Status PS 0 or 1
- Female or male patients aged ≥ 18 years (Japan ≥ 20 years) (South Korea ≥ 19 years).
- Adequate renal, liver, and bone marrow function.
- Resolved acute effects of any prior therapy to baseline severity or CTCAE Grade 1 except for adverse events (AEs) not constituting a safety risk by investigator judgment.
Who cannot join
- Unmanageable ascites (limited medical treatment to control ascites is permitted, but all participants with ascites require review by sponsor's medical monitor).
- Participants with any other active malignancy within 3 years prior to enrollment, except for adequately treated basal cell or squamous cell skin cancer, or carcinoma in situ.
- Major surgery, radiation therapy, or systemic anti-cancer therapy within 3 weeks prior to study entry.
- Prior irradiation to >25% of the bone marrow.
- ECG clinically relevant abnormalities (eg, QTc >470 msec, complete LBBB, second/third degree AV block, ST elevation or EKG changes suggesting myocardial infarction or active myocardia ischemia).
- Therapeutic anticoagulation. However, low molecular weight heparin is allowed. Vitamin K antagonists or factor Xa inhibitors may be allowed following discussion with the Sponsor.
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- Known or suspected hypersensitivity or severe allergy to active ingredient/excipients of PF-07248144.
- Active inflammatory GI disease, refractory and unresolved chronic diarrhea or previous gastric resection, lap band surgery or other GI conditions and surgeries that may significantly alter the absorption of PF-07248144 tablets. Gastroesophageal reflux disease under treatment is allowed.
- Pregnant or breastfeeding female participants.
Trial locations and contacts
43 sites in 5 countries. Contact the study team or a site near you to ask about taking part.
43 sites in 5 countries
United States22 sites, 20 recruiting
- Recruiting
MD Anderson The Woodlands
Conroe, Texas, 77384
- Recruiting
St. Elizabeth Healthcare
Edgewood, Kentucky, 41017
- Terminated
Holy Cross Hospital
Fort Lauderdale, Florida, 33308
- Recruiting
The University of Texas M. D. Anderson Cancer Center
Houston, Texas, 77030
- Recruiting
U.T. MD Anderson Cancer Center
Houston, Texas, 77030
- Recruiting
MD Anderson West Houston
Houston, Texas, 77079
- Recruiting
MD Anderson League City
League City, Texas, 77573
- Recruiting
Cedars-Sinai Cancer at Cedars-Sinai Medical Center
Los Angeles, California, 90048
- Recruiting
University Medical Center, lnc.:DBA University of Louisville Hospital
Louisville, Kentucky, 40202
- Recruiting
University of Louisville
Louisville, Kentucky, 40202
- Recruiting
UofL Health Brown Cancer Center
Louisville, Kentucky, 40202
- Recruiting
SCRI Oncology Partners
Nashville, Tennessee, 37203
- Recruiting
Smilow Cancer Hospital at Yale - New Haven
New Haven, Connecticut, 06510
- Recruiting
Yale-New Haven Hospital- Yale Cancer Center
New Haven, Connecticut, 06510
- Recruiting
Smilow Cancer Hospital Phase 1 Unit
New Haven, Connecticut, 06511
- Recruiting
Yale University
New Haven, Connecticut, 06511
- Recruiting
NEXT Oncology
San Antonio, Texas, 78229
- Recruiting
UCSF Medical Center at Mission Bay
San Francisco, California, 94158
- Terminated
HonorHealth
Scottsdale, Arizona, 85258
- Recruiting
Swedish Cancer Institute
Seattle, Washington, 98104
- Recruiting
Swedish Medical Center
Seattle, Washington, 98122
- Recruiting
MD Anderson
Sugar Land, Texas, 77478
Australia6 sites, 5 recruiting
- Recruiting
Cancer Research South Australia
Adelaide, South Australia, 5000
- Terminated
Chris O'Brien Lifehouse
Camperdown, New South Wales, 2050
- Recruiting
Peter MacCallum Cancer Centre
Melbourne, Victoria, 3000
- Recruiting
Royal Melbourne Hospital
Parkville, Victoria, 3050
- Recruiting
Western Health-Sunshine & Footscray Hospitals
St Albans, Victoria, 3021
- Recruiting
St. John of God Subiaco Hospital
Subiaco, Western Australia, 6008
South Korea6 sites, 6 recruiting
- Recruiting
Kyungpook National University Chilgok Hospital
Daegu, Taegu-kwangyǒkshi, 41404
- Recruiting
Seoul National University Bundang Hospital
Seongnam-si, Gyeonggi-do, 13620
- Recruiting
Seoul National University Hospital
Seoul, Seoul-teukbyeolsi [seoul], 03080
- Recruiting
Severance Hospital, Yonsei University Health System
Seoul, Seoul-teukbyeolsi [seoul], 03722
- Recruiting
Samsung Medical Center
Seoul, Seoul-teukbyeolsi [seoul], 06351
- Recruiting
Asan Medical Center
Seoul, 05505
China5 sites, 5 recruiting
- Recruiting
Beijing Cancer hospital
Beijing, Beijing Municipality, 100142
- Recruiting
Jilin Province Tumor Hospital
Changchun, Jilin, 130000
- Recruiting
Jilin Province Tumor Hospital
Changchun, Jilin, 132000
- Recruiting
SUN Yat-Sen University Cancer Center
Guangzhou, Guangdong, 510060
- Recruiting
The First Affiliated Hospital of Xi'an Jiaotong University
Xi'an, Shaanxi, 710061
Japan4 sites, 4 recruiting
- Recruiting
National Cancer Center Hospital
Chuo-ku, Tokyo, 104-0045
- Recruiting
National Cancer Center Hospital East
Kashiwa, Chiba, 277-8577
- Recruiting
Aichi Cancer Center Hospital
Nagoya, Aichi-ken, 464-8681
- Recruiting
Kanagawa cancer center
Yokohama, Kanagawa, 2418515
About this study
Official title: A PHASE 1/2A DOSE ESCALATION AND EXPANSION STUDY TO EVALUATE SAFETY, TOLERABILITY, PHARMACOKINETIC, PHARMACODYNAMIC, AND ANTI-TUMOR ACTIVITY OF PF-07248144 IN PARTICIPANTS WITH ADVANCED OR METASTATIC SOLID TUMORS
This is an open-label, multi center study to evaluate safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of PF-07248144 and early signs of clinical efficacy of PF-07248144 as a single agent and in combination with other agents
Read the detailed description
Study has two parts, Part 1 (dose escalation) and Part 2 (dose expansion). Part 1 is divided into Parts 1A, 1B, 1C, 1D and 1E and Part 2 is divided into Parts 2A, 2B, 2D and 2E. In Part 1A, single escalating doses of PF-07248144 alone will be administered to determine the maximum tolerable dose (MTD) and select the recommended dose for expansion (RDE). In Part 1B, 1C, 1D and 1E PF-07248144 will be administered in combination with either fulvestrant (Part 1B); palbociclib + letrozole (Part 1C) or PF-07220060+fulvestrant (Part 1D) or vepdegestrant (Part 1E). After the determination of the monotherapy RDE in Part 1A, PF-07248144 will be evaluated in a dose expansion cohort as a monotherapy in Part 2A.
After determination of the combination RDE from Part 1B, PF-07248144 in combination with fulvestrant, PF-07248144 will be evaluated in a combination dose expansion with fulvestrant in Part 2B. In Part 1C, PF-07248144 in combination with letrozole + palbociclib will be evaluated for dose finding to determine the MTD and RDE for this combination. After determination of the triple combination RDE from Part 1D, PF-07248144 in combination with PF-07220060 + fulvestrant will be evaluated in a combination dose-expansion cohort, Part 2D. After determination of the combination RDE from Part 1E, PF-07248144 in combination with vepdegestrant will be evaluated in a combination dose-expansion cohort, Part 2E.
- Conditions
- Locally Advanced or Metastatic ER+ HER2- Breast Cancer, Locally Advanced or Metastatic Castration-resistant Prostate Cancer, Locally Advanced or Metastatic Non-small Cell Lung Cancer
- Being tested
- PF-07248144, Fulvestrant, Letrozole, Palbociclib, PF-07220060
- Keywords
- Solid tumors
- Medical subject headings
- Carcinoma, Non-Small-Cell Lung
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
PF-07248144Drug
KAT6 Inhibitor
FulvestrantDrug
Also called Faslodex
Endocrine Therapy
LetrozoleDrug
Also called Femara
Endocrine Therapy
PalbociclibDrug
Also called Ibrance
CDK4/6 Inhibitor
PF-07220060Drug
CDK4 inhibitor
PF-07850327, ARV-471, vepdegestrantDrug
PROTAC (PROteolysis Targeting Chimera) ER degrader
| Study group | Role | What they receive |
|---|---|---|
| 1A Monotherapy Dose Escalation | Experimental | PF-07248144 Monotherapy Escalation Receives: Drug: PF-07248144 |
| 1B Combination Dose Escalation | Experimental | PF-07248144 with Fulvestrant Combination Dose Escalation Receives: Drug: PF-07248144; Drug: Fulvestrant |
| 1C Combination Dose Escalation | Experimental | PF-07248144 with Letrozole + Palbociclib Combination Dose Escalation Receives: Drug: PF-07248144; Drug: Letrozole; Drug: Palbociclib |
| 2A Monotherapy Dose Expansion Arm | Experimental | PF-07248144 Monotherapy Dose Expansion Receives: Drug: PF-07248144 |
| 2B Combination Dose Expansion Arm | Experimental | PF-07248144 with Fulvestrant Dose Expansion Receives: Drug: PF-07248144; Drug: Fulvestrant |
| 1D Combination Dose Escalation | Experimental | PF-07248144 with PF-07220060 +Fulvestrant Receives: Drug: PF-07248144; Drug: Fulvestrant; Drug: PF-07220060 |
| 2D Combination Dose Expansion Arm | Experimental | PF-07248144 with PF-07220060 +Fulvestrant Dose Expansion Receives: Drug: PF-07248144; Drug: Fulvestrant; Drug: PF-07220060 |
| China Monotherapy Dose Expansion | Experimental | PF-07248144 Monotherapy Dose Expansion Receives: Drug: PF-07248144 |
| 1E Combination Dose Escalation | Experimental | PF-07248144 with Vepdegestrant Combination Dose Escalation Receives: Drug: PF-07248144; Drug: PF-07850327, ARV-471, vepdegestrant |
| 2E Combination Dose Expansion Arm | Experimental | PF-07248144 with Vepdegestrant Combination Dose Expansion Receives: Drug: PF-07248144; Drug: PF-07850327, ARV-471, vepdegestrant |
What is being measured
The primary outcome is the main question the study is designed to answer.
Number of participants with dose-limiting toxicities in the Dose Escalation Arms.
Dose-limiting toxicities (DLTs)
Measured: Up to 29 days
Safety and Tolerability as assessed by adverse event monitoring for participants enrolled in the Dose Escalation Arms.
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Measured: Up to 24 months
Safety and Tolerability through monitoring of laboratory assessments for participants enrolled in the Dose Escalation Arms.
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
Measured: Up to 24 months
Safety and Tolerability as assessed by adverse event monitoring for participants enrolled in the Dose Expansion Arms
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Measured: Up to 24 months
Safety and Tolerability through monitoring of laboratory assessments for participants enroled in the Dose Expansion Arms
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
Measured: Up to 24 months
Secondary outcomes (23)
Single Dose: Maximum Observed Concentration (Cmax) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Single Dose: Time to Maximum concentration (Tmax) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Single Dose: AUC from time zero to time of last measurable concentration (AUClast) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Single and Multiple Dose: Terminal Elimination half-life (t1/2) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Multiple Dose: Steady-State Cmax (Cmax,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Multiple Dose: Steady-state Tmax (Tmax,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Multiple Dose: Steady state AUC during a dosage interval (τ) (AUCτ,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Multiple Dose: Steady-state Cmin (Cmin,ss) in the Dose Escalation and Dose Finding Arms.
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Multiple Dose: Steady-state apparent total clearance (CLss/F) in the Dose Escalation and Dose Finding Arms.
Pharmacokinetic (PK) assessments for PF-07248144, PF-07220060 (Part 1D) and vepdegestrant and ARV-473 (Part 1E)
Measured: Up to 24 months
Palbociclib trough concentrations at steady instate (Cmin,ss) in the 1C combination dose finding arm.
Pharmacokinetic (PK) assessment for palbociclib exposure.
Measured: Up to 24 months
Peak concentrations of PF-07248144, PF-07220060 (Part 2D) and vepdegestrant and ARV-473 (Part 2E) for selected cycles in the Dose Expansion Arms
Pharmacokinetic (PK) assessment for PF-07248144, PF-07220060 (Part 2D) and vepdegestrant and ARV-473 (Part 2E)
Measured: Up to 24 months
Trough concentrations of PF-07248144 for selected cycles in the Dose Expansion Arms
Pharmacokinetic (PK) assessment for PF-07248144 , PF-07220060 (Part 2D) and vepdegestrant and ARV-473 (Part 2E)
Measured: Up to 24 months
Maximum Observed Concentration (Cmax) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF-07248144.
Measured: Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
Time to Maximum concentration (Tmax) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF-07248144.
Measured: Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
AUC from time zero to time of last measurable concentration (AUClast) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF 07248144.
Measured: Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
Amount of PF-07248144 excreted in urine relative to dose administered (%) in a sub-set of participants in monotherapy dose expansion arm.
Evaluate urine pharmacokinetic (PK) of PF-07248144.
Measured: Up to 24 months
Renal clearance (CLr) in a sub-set of participants in monotherapy dose expansion arm
Evaluate urine pharmacokinetic (PK) of PF-07248144.
Measured: Up to 24 months
Progression Free Survival (PFS) observed in participants in the Dose Expansion Arms
Measured: Up to 24 months
Time to Progression (TTP) observed in participants enrolled in the Dose Expansion Arms
Measured: Up to 24 months
Overall survival (OS) observed in participants enrolled in Dose Expansion Arms
Measured: Up to 24 months
Best Overall Response (BOR) observed in participants in the dose expansion arms
Measured: Up to 24 months
Duration of Response (DOR) observed in participants in the dose expansion arms
Measured: up to 24 months
Clinical Benefit Rate (CBR) observed in participants in the Dose Expansion Arms
Measured: up to 24 months
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted28 Oct 2020
- Study start16 Nov 2020
- Primary completion27 Aug 2029 (estimated)
- Study completion27 Aug 2029 (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 Locally Advanced or Metastatic ER+ HER2- Breast CancerStudies of the same condition, open and under way.
- More trials run by PfizerThe 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 2
- Primary purpose
- Treatment
- Allocation
- Non-randomised
- Intervention model
- Sequential
- Model description
- The dose escalation parts and the dose finding parts of the study will be guided by a Bayesian analysis of Cycle 1 dose-limiting toxicity (DLT) data for PF-07248144 as monotherapy or in combination (Part 1B, Part 1C, Part 1D and Part 1E). A traditional 2-parameter Bayesian Logistic Regression Model (BLRM) will be used to model the DLT relationship of PF-07248144 monotherapy and a more complex BLRM model specifically designed for combinations will be used to model the dose/DLT relationship of PF-07248144 given in combination with fulvestrant, with letrozole + palbociclib, with PF-07220060 + fulvestrant or with vepdegestrant.
- Masking
- None (open label)
- Enrolment
- 320 participants (estimated)
Sponsor and investigators
- Lead sponsor
- Pfizer
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Pfizer CT.gov Call Center, Study director, Pfizer
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT04606446
- Sponsor's protocol ID
- C4551001
- Other IDs
- NCT04606446
- Acronym
- KAT6
- Status last verified
- Oct 2026
- First submitted
- 5 Oct 2020
- Last updated
- 21 Oct 2026
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- Yes: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical\_trials/trial\_data\_and\_results/data\_requests.
Publications
Mukohara T, Park YH, Sommerhalder D, Yonemori K, Hamilton E, Kim SB, Kim JH, Iwata H, Yamashita T, Layman RM, Mita M, Clay T, Chae YS, Oakman C, Yan F, Kim GM, Im SA, Lindeman GJ, Rugo HS, Liyanage M, Saul M, Le Corre C, Skoura A, Liu L, Li M, LoRusso PM. Inhibition of lysine acetyltransferase KAT6 in ER+HER2- metastatic breast cancer: a phase 1 trial. Nat Med. 2024 Aug;30(8):2242-2250. doi: 10.1038/s41591-024-03060-0. Epub 2024 Jun 1.
PubMed 38824244Bishop TR, Subramanian C, Bilotta EM, Garnar-Wortzel L, Ramos AR, Zhang Y, Asiaban JN, Ott CJ, Rock CO, Erb MA. Acetyl-CoA biosynthesis drives resistance to histone acetyltransferase inhibition. Nat Chem Biol. 2023 Oct;19(10):1215-1222. doi: 10.1038/s41589-023-01320-7. Epub 2023 May 1.
PubMed 37127754