HypercholesterolemiaPhase 1/2NCT03381287

A Multiple Ascending Dose Study of HTD1801 in Adults With Hypercholesterolemia

A Phase 1/2 study testing HTD1801 Tablets, 500 mg, HTD1801 Tablets, 1000 mg and HTD1801 Tablets, 2000 mg in people with Hypercholesterolemia, run by HighTide Therapeutics (Hong Kong) Limited at 3 sites in Australia.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record

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Trial summary

Who is it for?: Ages 18 to 70 years
Conditions the study is for: Hypercholesterolemia
What is being tested?: HTD1801 Tablets, 500 mg, HTD1801 Tablets, 1000 mg and HTD1801 Tablets, 2000 mg
Type of treatment: Pill or oral medicine
Could I receive a placebo?: Yes, some participants may receive a placebo
How many people: 50 participants
Where: 3 sitesAustralia
Study dates: 13 Apr 2018to 31 Dec 2018
Phase: Phase 1/2
Are there results?: Yes, posted in the registrySummary in the doctors' view

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 to 70 years
All sexes
No healthy volunteers
Adult, Older adult

Who may be able to join

Have given written informed consent
Males or females aged 18 to 70 years old at the time of first dosing
Have a body mass index (BMI) of >25.0 and ≤ 45.0 kg/m2 at Screening
Have a documented history of hypercholesterolemia, defined as LDL-C ≥ 2.59 mmol/L

Who cannot join

The use of any anti-dyslipidemia agent within 28 days prior to dosing
History of a total cholesterol ≥ 10.35 mmol/L or triglyceride ≥ 11.3 mmol/L
History of a clinically significant cardiac arrhythmia or clinically significant abnormal ECG results at Screening
Significant peripheral or coronary vascular disease
Clinically significant abnormal blood pressure at Screening or Baseline, defined as supine blood pressure ≥160/100 mmHg, or ≤ 90/60 mmHg
Primary hypothyroidism (thyroid stimulating hormone [TSH] > upper limit or normal [ULN] and free T4 < lower limit of normal [LLN]), primary subclinical hypothyroidism (screening TSH > ULN and free T4 within normal limits [WNL]), or secondary hypothyroidism (screening TSH < LLN and free T4< LLN) at Screening
Glucose-6-phosphate dehydrogenase (G6PD) deficiency

Trial locations and contacts

3 sites in 1 country.

Australia3 sites

CMAX Clinical Research Pty Ltd
Adelaide, South Australia, 5000
Q-Pharm Pty Ltd.
Herston, Queensland, 4006
Linear Clinical Research
Nedlands, Western Australia, 6009

Other trials in Australia

About this study

Official title: A Randomized, Double Blind, Placebo Controlled, Multicenter, Multiple Ascending Dose Study to Evaluate the Safety and Tolerability of HTD1801 in Adults With Hypercholesterolemia

This is a randomized, double-blind, placebo-controlled, multicenter, multiple ascending dose (MAD) study to evaluate the safety and tolerability, pharmacokinetic (PK), and pharmacodynamic (PD) profiles of HTD1801 in overweight to obese adults with hypercholesterolemia. There were 3 cohorts of dose levels as 500, 1000 and 2000 mg/day, with 16 subjects planned for each cohort randomized 3:1 to receive either HTD1801 or Placebo.

Conditions: Hypercholesterolemia
Being tested: HTD1801 Tablets, 500 mg, HTD1801 Tablets, 1000 mg, HTD1801 Tablets, 2000 mg, Placebo to match 500 mg HTD1801, Placebo to match 1000 mg HTD1801
Medical subject headings: Hypercholesterolemia

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

HTD1801 Tablets, 500 mgDrug
500 mg/day (250 mg BID)
HTD1801 Tablets, 1000 mgDrug
1000 mg/day (500 mg BID)
HTD1801 Tablets, 2000 mgDrug
2000 mg/day (1000 mg BID)
Placebo to match 500 mg HTD1801Drug
2 tablets/day (1 tablet BID)
Placebo to match 1000 mg HTD1801Drug
4 tablets/day (2 tablet BID)
Placebo to match 2000 mg HTD1801Drug
8 tablets/day (4 tablet BID)

Study groups in NCT03381287
Study group	Role	What they receive
HTD1801 250 mg BID	Experimental	Subjects received 500 mg/day HTD1801 Receives: Drug: HTD1801 Tablets, 500 mg
HTD1801 500 mg BID	Experimental	Subjects received 1000 mg/day HTD1801 Receives: Drug: HTD1801 Tablets, 1000 mg
HTD1801 1000 mg BID	Experimental	Subjects received 2000 mg/day HTD1801 Receives: Drug: HTD1801 Tablets, 2000 mg
Placebo	Placebo comparator	Not described Receives: Drug: Placebo to match 500 mg HTD1801; Drug: Placebo to match 1000 mg HTD1801; Drug: Placebo to match 2000 mg HTD1801

What is being measured

The primary outcome is the main question the study is designed to answer.

Number of Subjects With Treatment-Emergent Adverse Events (TEAEs)
TEAEs are defined as any AEs that commenced on or after exposure to study drug or any pre-existing AE that worsened in either intensity or frequency after exposure to study drug.
Measured: 4 weeks

Secondary outcomes (10)

Maximum Plasma Concentration (Cmax) of HTD1801 Components After Single-dose Oral Administration
Measured: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Maximum Plasma Concentration (Cmax) of HTD1801 Components After Multiple-dose Oral Administration
Measured: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Time to Maximum Plasma Concentration (Tmax) of HTD1801 Components After Single-dose Oral Administration
Measured: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Time to Maximum Plasma Concentration (Tmax) of HTD1801 Components After Multiple-dose Oral Administration
Measured: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Plasma Half-life of HTD1801 Components (T1/2) After Single-dose Oral Administration
Measured: 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Plasma Half-life of HTD1801 Components (T1/2) After Multiple-dose Oral Administration
Measured: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Percent Change in Low-density Lipoprotein-Cholesterol (LDL-C) From Baseline to Day 28 Within and Between Treatment Groups
Measured: Baseline, Day 14, Day 28
Percent Change in Triglycerides From Baseline to Day 28 Within and Between Treatment Groups
Measured: Baseline, Day 14, Day 28
Percent Change in Free-fatty Acids (FFA) From Baseline to Day 28 Within and Between Treatment Groups
Measured: Baseline, Day 14, Day 28
Percent Change in Lipoprotein-A From Baseline to Day 28 Within and Between Treatment Groups
Measured: Baseline, Day 14, Day 28

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

13 Apr 201831 Dec 2018

First posted21 Dec 2017
Study start13 Apr 2018
Primary completion31 Dec 2018
Study completion31 Dec 2018

Resources

Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
Publications (1)Papers the sponsor has linked to this study.
Other trials for HypercholesterolemiaStudies of the same condition, open and under way.
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 1/2
Primary purpose: Treatment
Allocation: Randomised
Intervention model: Sequential
Masking: Quadruple blind
Who is masked: Participant, Care provider, Investigator, Outcomes assessor
Enrolment: 50 participants (actual)

IDs, dates and publications

ClinicalTrials.gov ID: NCT03381287
Sponsor's protocol ID: HTD1801.PCT004
Status last verified: Aug 2026
First submitted: 18 Dec 2017
Last updated: 11 Aug 2026
Results posted: Yes, on ClinicalTrials.gov
FDA-regulated drug: No
FDA-regulated device: No

Publications

Di Bisceglie AM, Watts GF, Lavin P, Yu M, Bai R, Liu L. Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia. Lipids Health Dis. 2020 Nov 12;19(1):239. doi: 10.1186/s12944-020-01406-4.
PubMed 33183320

Want to know more?

The sponsor has not listed a contact. The official record may have more details.

Talk to your doctor first and take this page with you. Only the study team can confirm whether you can join.

Questions to ask the study team

What is the study trying to find out?
What would I need to do, and how often would I visit?
Could I receive a placebo instead of the treatment?
What are the possible risks and benefits for me?
Will it cost me anything? Are travel or time paid for?
Can I keep seeing my own doctor during the study?
What happens when the study ends?

See locations

Active, not recruitingObservational study
Study Evaluating LDL-C Change and Adherence to Inclisiran Lipid-lowering Therapy in ASCVD
Primary Hypercholesterolemia, Mixed Dyslipidemia
Active, not recruitingPhase 3
A Study of Inclisiran to Prevent Cardiovascular Events in High-risk Primary Prevention Patients.
Primary Prevention of Atherosclerotic Cardiovascular Disease
RecruitingObservational study
Causes and Natural History of Dyslipidemias
Hypercholesterolemia, Atherosclerosis
Active, not recruitingObservational study
Early Detection of Familial Hypercholesterolaemia in Pre-school Children ( CzeCH-IT)
Familial Hypercholesterolaemia
Not yet recruiting
Penn Family Screening for Familial Hypercholesterolemia (NHLBI R33) Trial 3
Familial Hypercholesterolemia

All Hypercholesterolemia trials

Study at a glance

From the registry record, last updated by the sponsor on 11 Aug 2026. Recruitment status is as the sponsor reported it: confirm with the study team.

Official title: A Randomized, Double Blind, Placebo Controlled, Multicenter, Multiple Ascending Dose Study to Evaluate the Safety and Tolerability of HTD1801 in Adults With Hypercholesterolemia
ClinicalTrials.gov ID: NCT03381287
Acronym / sponsor ID: HTD1801.PCT004
Conditions: Hypercholesterolemia
Phase: Phase 1/2
Study type: Interventional
Recruitment status: Completed
Enrolment: 50 participants (actual)
Lead sponsor: HighTide Therapeutics (Hong Kong) LimitedIndustry (pharma, biotech, devices)
Study start: 13 Apr 2018 (actual)
Primary completion: 31 Dec 2018 (actual)
Study completion: 31 Dec 2018 (actual)
First posted: 21 Dec 2017 (actual)
Results: Posted 3 Mar 2023

Clinical summary

The research question as the sponsor registered it. This describes what the study plans to test, not what it found.

Study design

Primary purpose: Treatment
Allocation: Randomised
Intervention model: Sequential
Masking: Quadruple blind (participant, care provider, investigator, outcomes assessor)
Number of arms: 4

Arm	Type	Receives
HTD1801 250 mg BID	Experimental	Drug: HTD1801 Tablets, 500 mgSubjects received 500 mg/day HTD1801
HTD1801 500 mg BID	Experimental	Drug: HTD1801 Tablets, 1000 mgSubjects received 1000 mg/day HTD1801
HTD1801 1000 mg BID	Experimental	Drug: HTD1801 Tablets, 2000 mgSubjects received 2000 mg/day HTD1801
Placebo	Placebo comparator	Drug: Placebo to match 500 mg HTD1801, Drug: Placebo to match 1000 mg HTD1801, Drug: Placebo to match 2000 mg HTD1801

Who may qualify

Ages: 18 to 70 years
Sex: All
Healthy volunteers: Not accepted
Age groups: Adult, Older adult

Key inclusion criteria (4 listed)

Have given written informed consent
Males or females aged 18 to 70 years old at the time of first dosing
Have a body mass index (BMI) of >25.0 and ≤ 45.0 kg/m2 at Screening
Have a documented history of hypercholesterolemia, defined as LDL-C ≥ 2.59 mmol/L

Key exclusion criteria (7 listed)

The use of any anti-dyslipidemia agent within 28 days prior to dosing
History of a total cholesterol ≥ 10.35 mmol/L or triglyceride ≥ 11.3 mmol/L
History of a clinically significant cardiac arrhythmia or clinically significant abnormal ECG results at Screening
Significant peripheral or coronary vascular disease
Clinically significant abnormal blood pressure at Screening or Baseline, defined as supine blood pressure ≥160/100 mmHg, or ≤ 90/60 mmHg

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
HTD1801 Tablets, 500 mg500 mg/day (250 mg BID)	Drug	HTD1801 250 mg BID
HTD1801 Tablets, 1000 mg1000 mg/day (500 mg BID)	Drug	HTD1801 500 mg BID
HTD1801 Tablets, 2000 mg2000 mg/day (1000 mg BID)	Drug	HTD1801 1000 mg BID
Placebo to match 500 mg HTD18012 tablets/day (1 tablet BID)	Drug	Placebo
Placebo to match 1000 mg HTD18014 tablets/day (2 tablet BID)	Drug	Placebo
Placebo to match 2000 mg HTD18018 tablets/day (4 tablet BID)	Drug	Placebo

Primary outcome

Number of Subjects With Treatment-Emergent Adverse Events (TEAEs)
Time frame: 4 weeks
TEAEs are defined as any AEs that commenced on or after exposure to study drug or any pre-existing AE that worsened in either intensity or frequency after exposure to study drug.

10 secondary outcomes

Maximum Plasma Concentration (Cmax) of HTD1801 Components After Single-dose Oral Administration
Time frame: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Maximum Plasma Concentration (Cmax) of HTD1801 Components After Multiple-dose Oral Administration
Time frame: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Time to Maximum Plasma Concentration (Tmax) of HTD1801 Components After Single-dose Oral Administration
Time frame: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Time to Maximum Plasma Concentration (Tmax) of HTD1801 Components After Multiple-dose Oral Administration
Time frame: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Plasma Half-life of HTD1801 Components (T1/2) After Single-dose Oral Administration
Time frame: 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 1
Plasma Half-life of HTD1801 Components (T1/2) After Multiple-dose Oral Administration
Time frame: 0. 0.25, 0.5, 1, 2, 3, 4, 8, 12 and 24 hours on Day 28
Percent Change in Low-density Lipoprotein-Cholesterol (LDL-C) From Baseline to Day 28 Within and Between Treatment Groups
Time frame: Baseline, Day 14, Day 28
Percent Change in Triglycerides From Baseline to Day 28 Within and Between Treatment Groups
Time frame: Baseline, Day 14, Day 28
Percent Change in Free-fatty Acids (FFA) From Baseline to Day 28 Within and Between Treatment Groups
Time frame: Baseline, Day 14, Day 28
Percent Change in Lipoprotein-A From Baseline to Day 28 Within and Between Treatment Groups
Time frame: Baseline, Day 14, Day 28

Results and safety

Results posted to the registry on 3 Mar 2023, as reported by the sponsor. Figures are copied from the record, not re-analysed. Full results on ClinicalTrials.gov.

Participant flow

Group	Started	Completed
Placebo	12	12
HTD1801 250 mg BID	12	11
HTD1801 500 mg BID	12	12
HTD1801 1000 mg BID	14	12

Primary outcome: Number of Subjects With Treatment-Emergent Adverse Events (TEAEs)

Time frame: 4 weeks. Count of participants. Unit: Participants

Measure	Placebo n = 12	HTD1801 250 mg BID n = 12	HTD1801 500 mg BID n = 12	HTD1801 1000 mg BID n = 14
TEAE	8	10	8	11
Serious TEAE	0	0	0	1
Severe TEAE	1	0	0	0
Drug-related TEAEs	4	2	7	6
TEAEs leading to treatment interrupted or discontinued	0	0	0	1

10 secondary outcomes are reported in the full results.

Adverse events

Time frame: 4 weeks. Other adverse events reported at 0% frequency or more

Group	Serious adverse events	Other adverse events	Deaths
Placebo	0 of 12 (0%)	8 of 12 (66.7%)	0 of 12
HTD1801 250 mg BID	0 of 12 (0%)	10 of 12 (83.3%)	0 of 12
HTD1801 500 mg BID	0 of 12 (0%)	8 of 12 (66.7%)	0 of 12
HTD1801 1000 mg BID	1 of 14 (7.1%)	11 of 14 (78.6%)	0 of 14

Loading the posted results from ClinicalTrials.gov…

Research links

Official record on ClinicalTrials.govLast updated by the sponsor 11 Aug 2026.
Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
Derived from this study: PubMed 33183320Di Bisceglie AM, Watts GF, Lavin P, Yu M, Bai R, Liu L. Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia. Lipids Health Dis. 2020 Nov 12;19(1):239. doi: 10.1186/s12944-020-01406-4.

Related trials for Hypercholesterolemia

Active, not recruitingObservational study
Study Evaluating LDL-C Change and Adherence to Inclisiran Lipid-lowering Therapy in ASCVD
Primary Hypercholesterolemia, Mixed Dyslipidemia
Active, not recruitingPhase 3
A Study of Inclisiran to Prevent Cardiovascular Events in High-risk Primary Prevention Patients.
Primary Prevention of Atherosclerotic Cardiovascular Disease
RecruitingObservational study
Causes and Natural History of Dyslipidemias
Hypercholesterolemia, Atherosclerosis
Active, not recruitingObservational study
Early Detection of Familial Hypercholesterolaemia in Pre-school Children ( CzeCH-IT)
Familial Hypercholesterolaemia
Not yet recruiting
Penn Family Screening for Familial Hypercholesterolemia (NHLBI R33) Trial 3
Familial Hypercholesterolemia

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.

Adrian Di Bisceglie, MD,FACP,FAASLD study director

HighTide Therapeutics USA, LLC

3 sites in 1 country: see every site and its status.

Questions about this trial

What is this clinical trial studying?

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 4 inclusion and 7 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: finished, as of the sponsor's last update on 11 Aug 2026. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 3 sites in Australia. 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. Some participants in this study may receive a placebo. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this combined 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.

Phase 2 studies give the treatment to a larger group to see whether it has the intended effect and to keep checking safety.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 3 Mar 2023). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

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?

Number of Subjects With Treatment-Emergent Adverse Events (TEAEs) (time frame: 4 weeks). 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 NCT03381287, which also lists 1 linked publication.

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 11 Aug 2026.