A Study to Evaluate the Relative Bioavailability of Pimicotinib Capsules Containing Free Base in Different Proportions in Healthy Subjects

Not Applicable

Active, not recruiting

• Conditions: Pharmacokinetics in Healthy Volunteers
• Interventions: Drug: pimicotinib capsules

• Registration Number: NCT07210996
• Lead Sponsor: Abbisko Therapeutics Co, Ltd

Brief Summary

This is an open-label, randomized, two-treatment, single-dose, two-way crossover study to evaluate the relative bioavailability and tolerability of Pimicotinib capsules containing free base in different proportions in healthy participants. 20 healthy participants are planned to be enrolled and will be evenly randomized to either Study Sequence A or Study Sequence B.Subjects in Sequence A/Sequence B will receive a single 50 mg oral dose of test/reference pimicotinib in period 1 and cross over in period 2. Blood samples will be collected for PK analysis in totally 32 time-points.

Detailed Description

Not available

Study Timeline

• Status Verified: 2025-09
• Study Start: 2025-09-12
• Study First Submitted: 2025-09-30
• Study First Submitted QC: 2025-09-30
• Last Update Submitted: 2025-09-30
• Primary Completion: 2025-10-06
• Study First Posted: 2025-10-07
• Last Update Posted: 2025-10-07
• Study Completion: 2025-10-30

Recruitment & Eligibility

• Status: ACTIVE_NOT_RECRUITING
• Sex: All
• Target Recruitment: 20

Inclusion Criteria

1. Healthy participants aged 18 to 50 years (inclusive) at screening and at least 25% of each sex should be included.

2. Weight ≥ 50.0 kg (male) or ≥ 45.0 kg (female), with a body mass index (BMI) between 18 and 28 (inclusive), BMI = weight (kg)/height (m)2;

3. Normal or abnormal but not clinically significant results in medical history, physical examination, clinical laboratory tests and other relevant examinations as assessed by the investigator at Screening;

4. Male or female participants of childbearing potential must agree to use effective methods of contraception during the study and within 6 months after the last dose of investigational product , and male participants should not donate sperm during such period; female participants should not donate ovum during such period and should not be pregnant or lactating. Pregnancy period is defined as the period from the date of conception until termination of pregnancy, and will be determined by laboratory test of human chorionic gonadotropin (hCG) within 7 days prior to initiation of the study;

5. Willing to participate in this study, understand the study procedures and sign the informed consent form prior to screening; willing to comply with the study procedures.

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Exclusion Criteria

1. Past or current medical history of chronic or severe conditions in cardiovascular, respiratory, blood, liver, kidney, gastrointestinal, endocrine or nervous systems;

2. Known or persistent mental disorders that may preclude the subject from participation in the study, as determined by the investigator;

3. Past history of gastric or intestinal surgery, or other operations (except for appendectomy) affecting the drug absorption;

4. Dysphagia and inability to take the investigational product orally;

5. Intolerant to venipuncture, difficult to collect blood samples, and fear of needle sickness and blood;

6. Known allergy to two or more kinds of foods and drugs; or allergic to pimicotinib or its excipients (lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, gelatin); and prone to allergic reactions such as rash and urticaria;

7. History of bacterial, fungal, parasitic, viral (excluding nasopharyngitis), mycobacterial infection, and COVID-19 infection within 30 days prior to screening; or abnormal chest X-ray (posteroanterior view) finding, assessed as clinically significant (by the investigator);

8. Symptoms of fatigue and pyrexia within 2 weeks prior to screening;

9. Abnormal laboratory tests: Alanine Aminotransferase (ALT) or Aspartate Aminotransferase (AST) > 1.2 × Upper Limit of Normal (ULN); Creatinine > 1.2 × ULN; Total Bilirubin (TBIL) > 1.5 × ULN; Creatine Kinase (CK) > 1.5 × ULN and amylase > 1.2 × ULN; hemoglobin <115g/L for Male or < 105g/L for Female;

10. Positive result for either of the following tests: serum Hepatitis B Surface Antigen (HBsAg), Hepatitis C Virus (HCV) antibody, Human Immunodeficiency Virus (HIV) antibody, and treponema pallidum antibody;

11. Participated in any clinical studies of drugs as a study subject and received the study drug within 3 months prior to screening;

12. Previously participated in any other study related to pimicotinib and received pimicotinib;

13. Used strong inhibitors or inducers of CYP3A4 within 14 days prior to screening and at Screening or intending to use during the study;

14. Have special diet requirements and cannot accept to take a unified dietary; specific dietary requirements the participants can only eat the food provided by the study site during hospitalization;

15. Consumption of more than 14 units of alcohol per week within 3 months prior to signing the informed consent form, or a positive result for alcohol breath test on the day pre-dose, or unable to abstain from alcohol during the study;

16. Consumption of more than 5 cigarettes per day within 3 months prior to signing the informed consent form, or unable to abstain from tobacco products during the study;

17. Previous chronic consumption of excessive amount of tea, coffee, or caffeinated beverages or unable to abstain from caffeinated beverages during the study;

18. Known history of drug abuse or positive for drug abuse screening test ;

19. Used over the counter or prescription drugs, including herbal medicine, health products, vitamins, and dietary supplements, within 14 days prior to screening, or plan to use such drugs during the study;

20. Donated or lost > 400 mL of blood within 3 months prior to screening; received blood transfusions or used blood products within 2 months prior to screening;

21. Received vaccine (including COVID-19 vaccine) within 2 months prior to screening, or plan to get vaccinated during the study;

22. Significant abnormalities and judged by the investigator as clinical significance in vital signs, including: forehead temperature > 37.6 °C; pulse rate > 100 beats/min or < 50 beats/min; systolic blood pressure ≥ 140 mmHg, diastolic blood pressure ≥ 90 mmHg;

23. Heart rate-corrected QT interval prolongation, QTcF > 470 ms (> 480 ms for females) (Note: QTc interval corrected using the Fridericia formula), or family history of long QT syndrome, or other clinically significant ECG abnormalities at Screening;

24. Participants involved in the design or conduct of this study and their immediate family members;

25. Participants who, in the opinion of the investigator, are not suitable for enrollment or may not be able to complete the study for other reasons.

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
pimicotinib (test capsule-reference capsule)	pimicotinib capsules	subjects in sequence A will receive a single oral dose of 50 mg test capsule administered as 2 x 25 mg (free base content at certain level) in period 1 day 1 and receive a single oral dose of 50 mg reference capsule administered as 2 x 25 mg (free base content below detection limit) in period 2 day 1.
pimicotinib (reference capsule-test capsule)	pimicotinib capsules	subjects in sequence B will receive a single oral dose of 50 mg reference capsule administered as 2 x 25 mg ((free base content below detection limit) in period 1 day 1 and receive a single oral dose of 50 mg test capsule administered as 2 x 25 mg (free base content at certain level) in period 2 day 1 .

Primary Outcome Measures

Name	Time	Method
Cmax	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours.	Peak concentration, the maximum observed plasma concentration of pimicotinib
AUC0-∞	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours.	Area under the plasma concentration-time curve of pimicotinib from time 0 to infinity, calculated as: AUC0-∞=AUClast +Clast/λz; Clast refers to the last measurable (non-BQL) plasma concentration of pimicotinib
AUClast	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours.	Area under the plasma concentration-time curve of pimicotinib from time 0 to the time of last measurable (non-BQL) concentration (calculated using the Linear Up Log Down trapezoidal method)

Secondary Outcome Measures

Name	Time	Method
AE	through study completion, an average of 26 days	To evaluate the safety following a single oral dose of the two different pimicotinib capsules under fasting conditions in healthy subjects,The relationship of each adverse event to the investigational product will be assessed by CTCAE v5.0.
t1/2	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours.	Elimination half-life
CL/F	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours	Total apparent clearance after a single oral dose
Vz/F	Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours	Apparent volume of distribution after a single oral dose

Trial Locations

Locations (1)

The First Hospital of Jilin University; 🇨🇳 Changchun, Jilin, China