A Study to Investigate The Effect of Pimicotinib on The Pharmacokinetics of Metformin, Fexofenadine and Rosuvastatin In Healthy Subjects

NCT06779253 | Completed Phase 1

• 1 other identifier: ABSK021-110
• Study Type: interventional
• Target: 39
• Locations: 1 country
• Sites: 1

Brief Summary

This is a an open-label, fixed-sequence DDI study conducted in Chinese healthy subjects to investigate the effect of multiple oral doses of pimicotinib on the pharmacokinetics of fexofenadine , rosuvastatin and metformin . Fexofenadine and rosuvastatin will be administered together as a cocktail, and metformin will be given via staggered dosing from the cocktail drugs administration. Approximately 38 healthy subjects will be enrolled to achieve 28 evaluable healthy subjects complete the study. Blood samples will be collected for PK analysis .

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (3)

• Cmax

  Peak concentration, the maximum observed plasma concentration of metformin, fexofenadine and rosuvastatin

  pre-dose, post-dose 0.5 hour, 1 hour, 1.5hours,2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10hours, 24 hours, 48 hours, 72 hours, 96 hours, 120 hours

• AUClast

  Area under the plasma concentration-time curve from time 0 to the time of last measurable concentration

  pre-dose, post-dose 0.5 hour, 1 hour, 1.5hours,2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10hours, 24 hours, 48 hours, 72 hours, 96 hours, 120 hours

• AUC0-∞

  Area under the plasma concentration-time curve from time 0 to infinity

  pre-dose, post-dose 0.5 hour, 1 hour, 1.5hours,2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10hours, 24 hours, 48 hours, 72 hours, 96 hours, 120 hours

Secondary Outcomes (1)

• AE

  through study completion, an average of 50 days

Study Arms (1)

Pimicotinib with Metformin, Fexofenadine and Rosuvastatin

OTHER

Multiple oral doses of pimicotinib (50 mg QD) on the pharmacokinetics of fexofenadine (P-gp sensitive substrate), rosuvastatin (BCRP sensitive substrate) and metformin (MATE1 sensitive substrate). Fexofenadine and rosuvastatin will be administered together as a cocktail, and metformin will be given via staggered dosing from the cocktail drugs administration.All subjects will receive the following study interventions:Day 1: metformin, Day 3: cocktail, Day 8 to 13: pimicotinib once daily (QD), Day 14: metformin + pimicotinib, Day 15: pimicotinib, Day 16: cocktail + pimicotinib, Day 17 to 20: pimicotinib QD

Drug: pimicotinib capsules

Interventions

pimicotinib capsules DRUG

the effect of multiple oral doses of pimicotinib (50 mg QD) on the pharmacokinetics of fexofenadine (P-gp sensitive substrate), rosuvastatin (BCRP sensitive substrate) and metformin (MATE1 sensitive substrate). Fexofenadine and rosuvastatin will be administered together as a cocktail, and metformin will be given via staggered dosing from the cocktail drugs administration

Pimicotinib with Metformin, Fexofenadine and Rosuvastatin

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy subjects aged 18 to 50 years (inclusive) at screening and at least 25% of each sex should be included.
• Weight ≥ 50.0 kg (male) or ≥ 45.0 kg (female), with a body mass index (BMI) between 18.0 and 28.0 (inclusive), BMI = weight (kg)/height (m)2;
• Normal or abnormal but not clinically significant results in physical examination, clinical laboratory tests and other relevant examinations as assessed by the investigator at Screening;
• Male or female subjects 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 subjects should not donate sperm during such period; female subjects 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) during medical examination and baseline prior to initiation of the study;
• 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.

You may not qualify if:

• Past or current medical history of chronic or severe conditions in cardiovascular, respiratory, blood, liver, kidney, gastrointestinal, endocrine or nervous systems;
• Known or persistent mental disorders that may preclude the participant from participation in the study, as determined by the investigator;
• Past history of gastric or intestinal surgery, or other operations (except for appendectomy) affecting the drug absorption;
• Dysphagia or inability to take the investigational product orally;
• Intolerant to venipuncture, difficult to collect blood samples, or fear of needle sickness and blood;
• Known allergy to two or more kinds of foods and drugs; or allergic to fexofenadine, rosuvastatin, metformin or pimicotinib or its excipients (lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, gelatin, titanium dioxide); and prone to allergic reactions such as rash and urticaria;
• 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 finding, assessed as clinically significant (by the investigator);
• Symptoms of fatigue and pyrexia within 2 weeks prior to screening;
• Abnormal laboratory tests;
• 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;
• Participated in any clinical studies of drugs as a study participant and received the study drug within 3 months prior to screening;
• Previously participated in any other study related to pimicotinib and received pimicotinib;
• Used strong inhibitors or inducers of CYP3A4(including grapefruit juice, grapefruit hybrids, punica granatum, carambola, citrus maxima, and Seville oranges) and transporter P-gp/BCRP/MATE1/OATP1B1/OATP1B3/MATE2-K/OCT2 inhibitors within 14 days prior to screening and at Screening or intending to use during the study;
• Have special dietary requirements or cannot accept to take a unified diet; specific dietary requirements: the subjects can only eat the food provided by the study site during hospitalization;
• Consumption of more than 14 units of alcohol per week (1 unit of alcohol = about 360 mL of beer or 45 mL of spirits containing 40% alcohol or 150 mL of wine) within 3 months prior to signing the informed consent form, or a positive result for alcohol breath test on the day pre-dose (breath alcohol content \> 0.0 mg/100 mL), or unable to abstain from alcohol during the study;

Sponsors & Collaborators

• Abbisko Therapeutics Co, Ltd: lead

Study Sites (1)

The First Affiliated Hospital Shandong First Medical University (Shandong Provincial Qianfoshan Hospital)

Jinan, Shandong, 250014, China

Location

Study Officials

• Wei Zhao, Doctor

  The First Affiliated Hospital Shandong First Medical University (Shandong Provincial Qianfoshan Hospital)

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Fexofenadine and rosuvastatin will be administered together as a cocktail, and metformin will be given via staggered dosing from the cocktail drugs administration. All subjects will receive the following study interventions:Day 1: metformin； Day 3: cocktail；Day 8 to 13: pimicotinib once daily (QD)；Day 14: metformin + pimicotinib；Day 15: pimicotinib，Day 16: cocktail + pimicotinib，Day 17 to 20: pimicotinib QD

Study Record Dates

• First Submitted: January 9, 2025
• First Posted: January 16, 2025
• Study Start: March 14, 2025
• Primary Completion: April 4, 2025
• Study Completion: May 22, 2025
• Last Updated: June 26, 2025

Record last verified: 2025-06

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)