A Study to Investigate the Effect of Rifampicin on the Uptake and Breakdown of ACT-246475 in Healthy Subjects

NCT03814200 | Completed Phase 1 FDA Drug

• 2 other identifiers: ID-076-1062018-004226-28
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

The study will investigate the effect of rifampicin on the uptake and breakdown of ACT-246475 in healthy subjects

Conditions

Healthy Subject

Outcome Measures

Primary Outcomes (5)

• Area under the plasma concentration-time curve (AUC) from time zero to time t of the last measured concentration above the limit of quantification (AUC0-t)

  The plasma PK parameters of ACT-246475 will be derived by non-compartmental analysis of the plasma concentration-time profiles

  Up to 36 hours after treatment administration

• AUC from zero to infinity (AUC0-inf)

  The plasma PK parameters of ACT-246475 will be derived by non-compartmental analysis of the plasma concentration-time profiles

  Up to 36 hours after treatment administration

• The maximum plasma concentration (Cmax)

  The plasma PK parameters of ACT-246475 will be derived by non-compartmental analysis of the plasma concentration-time profiles

  Up to 36 hours after treatment administration

• The time to reach Cmax (tmax)

  The plasma PK parameters of ACT-246475 will be derived by non-compartmental analysis of the plasma concentration-time profiles

  Up to 36 hours after treatment administration

• Terminal half-life (t½)

  The plasma PK parameters of ACT-246475 will be derived by non-compartmental analysis of the plasma concentration-time profiles

  Up to 36 hours after treatment administration

Study Arms (2)

Treatment period A

EXPERIMENTAL

Treatment A1: saline 0.9% followed by Treatment A2: ACT-246475

Drug: Saline; Drug: ACT-246475

Treatment period B

EXPERIMENTAL

Treatment B1: rifampicin followed by Treatment B2: ACT-246475

Drug: ACT-246475; Drug: Rifampicin

Interventions

Saline DRUG

Single i.v. infusion of 100 mL saline 0.9% for 30 min

Treatment period A

ACT-246475 DRUG

Single s.c. dose of 4 mg ACT-246475 in the thigh under fasting conditions

Also known as: Selatogrel

Treatment period A; Treatment period B

Rifampicin DRUG

Single i.v. infusion of 600 mg rifampicin (100 mL) for 30 min

Treatment period B

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Signed informed consent in a language understandable to the subject prior to any study-mandated procedure
• Healthy male and female subjects aged between 18 and 65 years (inclusive) at Screening
• Body mass index of 18.0 to 30.0 kg/m2 (inclusive) at Screening
• Systolic blood pressure 100-145 mmHg, diastolic blood pressure 50-90 mmHg, and pulse rate 45-90 bpm (inclusive), measured on the same arm, after 5 min in the supine position at screening and on Day -1 of the first period
• Hematology and coagulation test results not deviating from the normal range to a clinically relevant extent at Screening and on Day -1 of the first period
• Women of childbearing potential must have a negative serum pregnancy test at Screening and a negative urine pregnancy test on Day- 1 of the first treatment period and must agree to consistently and correctly use a highly effective method of contraception

You may not qualify if:

• Previous exposure to ACT-246475.
• Previous exposure to rifampicin within 3 months prior to Screening.
• Known hypersensitivity to P2Y12 receptor antagonists or rifampicin, or to any of the rifamycins, or any of their excipients
• Loss of 250 mL or more of blood within 3 months prior to Screening
• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol
• Family or personal history of prolonged bleeding (e.g., after surgical intervention) or bleeding disorders (e.g., thrombocytopenia, clotting disturbances), intracranial vascular diseases, stroke, reasonable suspicion of vascular malformations, or peptic ulcers
• Known platelet disorders (e.g., Glanzmann thromboasthenia, von Willebrand disease, platelet release defect)

Sponsors & Collaborators

• Viatris Innovation GmbH: lead

Study Sites (1)

QPS Netherlands B.V.

Groningen, 9700, Netherlands

Location

Related Publications (1)

• Schilling U, Dingemanse J, Voors-Pette C, Romeijn C, Dogterom P, Ufer M. Effect of Rifampin-Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel. Clin Transl Sci. 2020 Sep;13(5):886-890. doi: 10.1111/cts.12774. Epub 2020 Mar 31.

  PMID: 32166864 RESULT

MeSH Terms

Interventions

Sodium Chloride; selatogrel; Rifampin

Intervention Hierarchy (Ancestors)

Chlorides; Hydrochloric Acid; Chlorine Compounds; Inorganic Chemicals; Sodium Compounds; Rifamycins; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds

Study Officials

• Clinical Trials

  Viatris Innovation GmbH

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 21, 2019
• First Posted: January 23, 2019
• Study Start: January 3, 2019
• Primary Completion: February 12, 2019
• Study Completion: February 19, 2019
• Last Updated: July 3, 2025

Record last verified: 2022-11

Data Sharing

• IPD Sharing: Will not share

Locations

NL (1)