Mass Balance and Pharmacokinetics Study of Derazantinib in Healthy Male Subjects

NCT ID: NCT04098692

Last Updated: 2021-01-19

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 12 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2019-08-08
• Study Completion Date: 2019-11-18

Brief Summary

This is a Phase 1, two-part, open-label, single centre, single arm study in healthy male subjects to investigate the oral PK, intravenous (IV) PK, mass balance, bioavailability and metabolites profiling and identification of derazantinib.

Conditions

Healthy Volunteers

Study Design

• Allocation Method: NA
• Intervention Model: SINGLE_GROUP
• Primary Study Purpose: OTHER
• Blinding Strategy: NONE

Study Groups

Single-Arm: Derazantinib (Part 1 and Part 2)

• Part 1: 300 mg Derazantinib oral administration followed by 100 μg [14C]-Derazantinib intravenous microdose
• Part 2: 300 mg [14C]-Derazantinib oral administration

Group Type: EXPERIMENTAL

Derazantinib capsule

Intervention Type: DRUG

300 mg derazantinib oral administration (3x100 mg capsules)

[14C]-Derazantinib solution for infusion

Intervention Type: DRUG

100 μg \[14C\]-derazantinib intravenous administration

[14C]-Derazantinib capsule

Intervention Type: DRUG

300 mg \[14C\]-derazantinib oral administration (3x100 mg capsules)

Interventions

Derazantinib capsule

300 mg derazantinib oral administration (3x100 mg capsules)

Intervention Type: DRUG

[14C]-Derazantinib solution for infusion

100 μg \[14C\]-derazantinib intravenous administration

Intervention Type: DRUG

[14C]-Derazantinib capsule

300 mg \[14C\]-derazantinib oral administration (3x100 mg capsules)

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Healthy males
• Age 18 to ≤ 55 years (Part 1)
• Age 30 to ≤ 65 years (Part 2)
• Body mass index of 18.0 to 29.0 kg/m² and a minimum body weight of 50 kg
• Must have regular bowel movements
• Must agree to adhere to the contraception requirements

Exclusion Criteria

• Male subjects with pregnant partners
• Subjects who have received any investigational medicine in a clinical research study within the previous 3 months
• Subjects who are study site employees, or immediate family members of a study site or sponsor employee
• History of any drug or alcohol abuse in the 12 months prior to dosing
• Regular alcohol consumption in males > 21 units per week
• Smokers and users of e-cigarettes and nicotine replacement products and those who have used these products within the last 3 months
• Radiation exposure (diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 2017, shall participate in the study
• Participation in any study involving administration of any [14C]-labelled compound within 12 months prior to screening (Part 1 only)
• Excessive caffeine consumption within 14 days prior to screening, defined as 800 mg per day (approximately 6 large cups of coffee)
• Subjects who do not have suitable veins
• Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the Investigator
• Confirmed positive drugs of abuse test result
• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results, or history of immunodeficiency diseases, including a positive HIV (ELISA and western blot) test result
• Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance of < 70 mL/min using the Cockcroft-Gault equation
• History of clinically significant cardiovascular, renal, hepatic, chronic respiratory or gastrointestinal disease, neurological or psychiatric disorder or current clinical evidence of any corneal or retinal disorder
• Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active
• Known hypersensitivity or allergy to natural rubber latex
• History of any food allergies
• History of clinically significant ECG abnormalities
• Familial history of sick-sinus syndrome
• Recent (within the last 3 years) and/or recurrent history of autonomic dysfunction
• Recent (within the last 3 years) and/or recurrent history of acute or chronic bronchospastic disease (including asthma disease, treated or not treated)
• History of malignancy of any organ system (other than localised basal cell carcinoma of the skin), treated or untreated, within the past 5 years
• Use of any prescription drugs (including vaccines), herbal supplements (such as St. John's Wort, homeopathic preparations), within 4 weeks prior to initial dosing, and/or over-the-counter medication, dietary supplements (vitamins and minerals included) within 2 weeks prior to initial dosing
• Donation or loss of 400 mL or more of blood and/or plasma within 3 months prior to initial dosing
• Any history or presence of frequent episodes of diarrhoea (defined as an increase of 4 to 6 stools per day over usual individual defecation pattern).
• Significant illness within 2 weeks prior to initial dosing
• Any surgical or medical condition which might significantly alter the absorption, distribution, metabolism, or excretion of drugs, or which may jeopardise the subject in case of participation in the study.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 65 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Basilea Pharmaceutica

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Nand Singh, MD

Role: PRINCIPAL_INVESTIGATOR

Quotient Sciences

Locations

Quotient Sciences, Ruddington

Nottingham, , United Kingdom

Countries

United Kingdom

Other Identifiers

DZB-CS-102

Identifier Type: -

Identifier Source: org_study_id