A Comparative Study of Selatogrel (ACT-246475) Formulations in Healthy Subjects

NCT04557280 | Completed Phase 1 FDA Drug FDA Device

• 1 other identifier: ID-076-105
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

The main purpose is to study the pharmacokinetics of selatogrel (ACT-246475) using different administration modes and formulations. The clinical pharmacology data will be used to support demonstration of bioequivalence and interchangeability of the different formulations.

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (5)

• Area under the plasma concentration-time curve (AUC0-t) of selatogrel

  Multiple pharmacokinetic sampling at predefined times on Day 1 (pre-dose) up to Day 3.

• The area under the plasma concentration-time curve from zero to infinity (AUC0-inf) of selatogrel

  Multiple pharmacokinetic sampling at predefined times on Day 1 (pre-dose) up to Day 3.

• The maximum plasma concentration (Cmax) of selatogrel

  Multiple pharmacokinetic sampling at predefined times on Day 1 (pre-dose) up to Day 3.

• Time to reach Cmax (tmax)

  Multiple pharmacokinetic sampling at predefined times on Day 1 (pre-dose) up to Day 3.

• Terminal half-life (t½) of selatogrel

  Multiple pharmacokinetic sampling at predefined times on Day 1 (pre-dose) up to Day 3.

Secondary Outcomes (7)

• Change from baseline in systolic and diastolic supine blood pressure

  Multiple predefined times on Day 1 (pre-dose) up to Day 3.

• Change from baseline in pulse rate

  Multiple predefined times on Day 1 (pre-dose) up to Day 3.

• Change from baseline in body weight

  Multiple predefined times on Day 1 (pre-dose) up to Day 3.

• Change from baseline in the electric activity of the heart (12-lead electrocardiogram)

  Multiple predefined times on Day 1 (pre-dose) up to Day 3.

• Change from baseline in coagulation laboratory tests

  Multiple predefined times on Day 1 (pre-dose) up to Day 3.

Study Arms (3)

Treatment A: liquid formulation via auto-injector

EXPERIMENTAL

Selatogrel will be administered as a liquid formulation in a sealed prefilled syringe in an auto-injector forming an integral ready-to-use single-dose drug delivery system.

Combination Product: Selatogrel

Treatment B: liquid formulation via syringe

EXPERIMENTAL

Selatogrel will be administered as a liquid formulation in a sealed prefilled syringe.

Combination Product: Selatogrel

Treatment C: lyophilizate-based formulation via syringe

EXPERIMENTAL

Selatogrel will be administered as a reconstituted lyophilizate-based formulation for injection.

Drug: Selatogrel

Interventions

Selatogrel COMBINATION_PRODUCT

A single subcutaneous injection of 16 mg.

Also known as: ACT-246475

Treatment A: liquid formulation via auto-injector; Treatment B: liquid formulation via syringe

Eligibility Criteria

• Age: 18 Years - 59 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Signed informed consent in a language understandable to the participant prior to any study-mandated procedure.
• Healthy male or female participant aged between 18 and 59 years (inclusive) at screening.
• Body mass index of 18.0 to 31.9 kg/m2 (inclusive) at screening and a minimum weight of 50.0 kg at screening and on Day -1.
• Systolic blood pressure 100 to 140 mmHg, diastolic blood pressure 50 to 90 mmHg, and pulse rate 45 to 100 bpm (inclusive), measured on the left arm, after 5 minutes in the supine position at screening and Day-1.
• lead electrocardiogram (ECG) without clinically relevant abnormalities, measured after 5 min in the supine position at screening and on Day-1.
• Clinical laboratory values are within the standard normal ranges or determined to be clinically insignificant in the opinion of the investigator at screening and on Day -1.
• Women must have a negative serum pregnancy test at screening and a negative urine pregnancy test at baseline (i.e., Day -1 of the first period). Women of childbearing potential must consistently and correctly use (from screening, during the entire study, and for at least 30 days after last study treatment injection) an acceptable effective method of contraception, be sexually inactive, or have a vasectomized partner. If a hormonal contraceptive is used, it must be initiated at least 1 month before first treatment administration.
• Women of non-childbearing potential.

You may not qualify if:

• Pregnant or lactating woman.
• Previous exposure to selatogrel (ACT-246475).
• Previous treatment with acetylsalicylate, non-steroidal anti-inflammatory drugs, P2Y12 receptor antagonists, or any medication with blood-thinning activity (i.e., injectable or oral anticoagulants) within 3 weeks prior to study treatment administration.
• Treatment with another investigational small molecule drug within 30 days or 5 x terminal half-lives (\[t½\], whichever is longer) or with an investigational biologic drug within 90 days prior to screening.
• Known hypersensitivity to P2Y12 receptor antagonists or to excipients used in any of the formulations.
• History or clinical evidence of alcoholism or drug abuse within 3 years prior to screening.
• History of major medical or surgical disorders, which, in the opinion of the investigator, are likely to interfere with the absorption, distribution, metabolism or excretion of the study treatment (appendectomy and herniotomy allowed, cholecystectomy not allowed).
• Family or personal history of prolonged bleeding (e.g., after surgical intervention) or bleeding disorders (e.g., thrombocytopenia, clotting disturbances), intracranial vascular diseases, stroke, transient ischemic attack, reasonable suspicion of vascular malformations, peptic ulcers.
• Platelet count less than 120 x10\^9 per litre at screening and on Day-1.
• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.

Sponsors & Collaborators

• Viatris Innovation GmbH: lead

Study Sites (1)

Altasciences Clinical Kansas, Inc

Overland Park, Kansas, 66212, United States

Location

Related Publications (1)

• Zenklusen I, Hsin CH, Schilling U, Kankam M, Krause A, Ufer M, Dingemanse J. Transition from Syringe to Autoinjector Based on Bridging Pharmacokinetics and Pharmacodynamics of the P2Y12 Receptor Antagonist Selatogrel in Healthy Subjects. Clin Pharmacokinet. 2022 May;61(5):687-695. doi: 10.1007/s40262-021-01097-9. Epub 2021 Dec 28.

  PMID: 34961905 RESULT

MeSH Terms

Interventions

selatogrel

Study Officials

• Clinical Trials

  Viatris Innovation GmbH

  STUDY DIRECTOR

Study Design

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

Model Details: Single-center, randomized, 3-period crossover.

Study Record Dates

• First Submitted: September 7, 2020
• First Posted: September 21, 2020
• Study Start: November 6, 2020
• Primary Completion: December 19, 2020
• Study Completion: December 19, 2020
• Last Updated: July 3, 2025

Record last verified: 2022-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)