Potential Drug Interaction Study Between Vemircopan and Rosuvastatin, Metformin, Levonorgestrel/Ethinyl Estradiol-containing Oral Contraceptives, and Carbamazepine

NCT06071442 | Completed Phase 1 FDA Drug

• 2 other identifiers: D7841C00012ALXN2050-HV-111
• Study Type: interventional
• Target: 60
• Locations: 1 country
• Sites: 1

Brief Summary

This study will investigate the potential drug interactions between vemircopan and metformin, rosuvastatin, levonorgestrel/ ethinyl estradiol (LNG/EE)-containing oral contraceptive(s) (OCs), and carbamazepine in healthy participants.

Conditions

Healthy Participants

Keywords

Drug-drug interaction; Pharmacokinetic

Outcome Measures

Primary Outcomes (15)

• Part 1: Maximum observed plasma (peak) concentration (Cmax) of Metformin

  Cmax for single-dose metformin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of metformin.

  Up to 48 hours post-dose

• Part 1: AUC from time zero to the last quantifiable concentration (AUCt) of Metformin

  AUCt for single-dose metformin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of metformin.

  Up to 48 hours post-dose

• Part 1: AUC from time zero extrapolated to infinity (AUC∞) of Metformin

  Cmax for single-dose metformin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of metformin.

  Up to 48 hours post-dose

• Part 1: Cmax of Rosuvastatin

  Cmax for single-dose rosuvastatin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of rosuvastatin.

  Up to 96 hours post-dose

• Part 1: AUCt of Rosuvastatin

  AUCt for single-dose rosuvastatin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of rosuvastatin.

  Up to 96 hours post-dose

• Part 1: AUC∞ of Rosuvastatin

  Cmax for single-dose rosuvastatin without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of rosuvastatin.

  Up to 96 hours post-dose

• Part 2: Cmax of LNG

  Cmax for single-dose LNG without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of LNG.

  Up to 120 hours post-dose

• Part 2: AUCt of LNG

  AUCt for single-dose LNG without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of LNG.

  Up to 120 hours post-dose

• Part 2: AUC∞ of LNG

  Cmax for single-dose LNG without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of LNG.

  Up to 120 hours post-dose

• Part 2: Cmax of EE

  Cmax for single-dose EE without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of EE.

  Up to 120 hours post-dose

• Part 2: AUCt of EE

  AUCt for single-dose EE without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of EE.

  Up to 120 hours post-dose

• Part 2: AUC∞ of EE

  Cmax for single-dose EE without and with co-administration with vemircopan will be assessed to determine the effect of multiple doses of vemircopan on the single-dose PK of EE.

  Up to 120 hours post-dose

• Part 3: Cmax of Vemircopan

  Cmax for single-dose vemircopan without and with co-administration with carbamazepine will be assessed to determine the effect of multiple doses of carbamazepine on the single-dose PK of vemircopan.

  Up to 72 hours post-dose

• Part 3: AUCt of Vemircopan

  AUCt for single-dose vemircopan without and with co-administration with carbamazepine will be assessed to determine the effect of multiple doses of carbamazepine on the single-dose PK of vemircopan.

  Up to 72 hours post-dose

• Part 3: AUC∞ of Vemircopan

  Cmax for single-dose vemircopan without and with co-administration with carbamazepine will be assessed to determine the effect of multiple doses of carbamazepine on the single-dose PK of vemircopan.

  Up to 72 hours post-dose

Secondary Outcomes (40)

• Part 1: Number of participants with Treatment Emergent Adverse Events

  From Screening (Day -28 to Day -2) up to follow-up Visit or early discontinuation visit (approximately 57 days)

• Part 2: Number of participants with Treatment Emergent Adverse Events

  From Screening (Day -28 to Day -2) up to follow-up Visit or early discontinuation visit (approximately 54 days)

• Part 3: Number of participants with Treatment Emergent Adverse Events

  From Screening (Day -28 to Day -2) up to follow-up Visit or early discontinuation visit (approximately 63 days)

• Part 1: Time corresponding to the occurrence of Cmax (tmax) of Metformin

  Up to 48 hours post-dose

• Part 1: Apparent terminal elimination half-life (t½) of Metformin

  Up to 48 hours post-dose

Study Arms (3)

Part 1: Vemircopan, Metformin and Rosuvastatin

EXPERIMENTAL

Participants will receive Vemircopan, Metformin and Rosuvastatin in a fixed sequence over 2 periods. Period 1 (8 days): Participants will receive a single dose of metformin on day 1 and a single dose of rosuvastatin on day 4. Period 2 (12 days): Participants will receive vemircopan twice daily from day 1 to day 11. On day 5, participants will receive metformin co-administered with vemircopan. On day 8, participants will receive rosuvastatin co-administered with vemircopan. There will be a washout period of at least 4 days between the dose of rosuvastatin in Period 1 and the first dose of vemircopan in Period 2.

Drug: Vemircopan; Drug: Rosuvastatin; Drug: Metformin

Part 2: Vemircopan and LNG/EE-Containing OCs

EXPERIMENTAL

Participants will receive Vemircopan and LNG/EE-Containing OCs in a fixed sequence over 2 periods. Period 1 (7 days): Participants will receive a single dose of OC, consisting of LNG and EE on day 1. Period 2 (10 days): Participants will receive multiple doses of vemircopan from day 1 to day 9. On day 5, participants will receive a single dose of OC co-administered with vemircopan. There will be a washout period of at least 7 days between the dose of OC in Period 1 and the first dose of vemircopan in Period 2.

Drug: Vemircopan; Drug: Levonorgestrel / Ethinyl Estradiol

Part 3: Vemircopan and Carbamazepine

EXPERIMENTAL

Participants will receive Vemircopan and Carbemazepine in a fixed sequence over 2 periods. Period 1 (4 days): Participants will receive a single oral dose of vemircopan on day 1. Period 2 (22 days): Participants will receive carbemazepine twice daily from day 1 to day 21. On day 19, participants will receive a single oral dose of vemircopan co-administered with carbamazepine. There will be a washout period of at least 4 days between the dose of vemircopan in Period 1 and the first dose of carbamazepine in Period 2.

Drug: Vemircopan; Drug: Carbamazepine

Interventions

Vemircopan DRUG

Participants will receive oral tablets of Vemircopan.

Also known as: ALXN2050

Part 1: Vemircopan, Metformin and Rosuvastatin; Part 2: Vemircopan and LNG/EE-Containing OCs; Part 3: Vemircopan and Carbamazepine

Rosuvastatin DRUG

Participants will receive oral coated tablets of Rosuvastatin.

Part 1: Vemircopan, Metformin and Rosuvastatin

Metformin DRUG

Participants will receive oral film-coated tablets of Metformin.

Part 1: Vemircopan, Metformin and Rosuvastatin

Levonorgestrel / Ethinyl Estradiol DRUG

Participants will receive oral tablets of Levonorgestrel/ Ethinyl Estradiol.

Also known as: SIMPESSE

Part 2: Vemircopan and LNG/EE-Containing OCs

Carbamazepine DRUG

Participants will receive oral chewable tablets of Carbamazepine.

Part 3: Vemircopan and Carbamazepine

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants who are medically healthy with no clinically significant or relevant abnormalities as determined by medical history, physical or neurological examination, vital signs, 12-lead ECG, screening clinical laboratory profiles (hematology, biochemistry, coagulation, and urinalysis), as deemed by the Investigator or designee.
• Body weight of at minimum 50 kg and body mass index (BMI) within the range 18 to 32 kg/m\^2 (inclusive) at the Screening.
• Male and female participants should adhere to the protocol defined contraceptive methods.

You may not qualify if:

• History or presence of medical (eg, cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrinological, hematological, neurological or other disorders) or psychiatric conditions or diseases.
• History of clinically significant hypersensitivity or idiosyncratic reaction to the study drugs or related compounds.
• History of drug or alcohol abuse within 2 years prior to first dosing
• Current tobacco users or smokers (defined as any tobacco or nicotine-containing product use within 3 months prior to first dosing).
• Donation of whole blood from 3 months prior to first dose administration, or of plasma from 30 days before first dose administration.
• Female participants who have a positive pregnancy test at Screening or Day -1, or who are lactating.
• Positive drugs of abuse, cotinine, or alcohol screen at Screening or Day -1.

Sponsors & Collaborators

• Alexion Pharmaceuticals, Inc.: lead

Study Sites (1)

Research Site

Brooklyn, Maryland, 21225, United States

Location

MeSH Terms

Interventions

Rosuvastatin Calcium; Metformin; Ethinyl Estradiol-Norgestrel Combination; Carbamazepine

Intervention Hierarchy (Ancestors)

Sulfonamides; Amides; Organic Chemicals; Fluorobenzenes; Hydrocarbons, Fluorinated; Hydrocarbons, Halogenated; Hydrocarbons; Sulfones; Sulfur Compounds; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Biguanides; Guanidines; Amidines; Ethinyl Estradiol; Norpregnatrienes; Norpregnanes; Norsteroids; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Norgestrel; Norpregnenes; Estrogenic Steroids, Alkylated; Estradiol Congeners; Gonadal Steroid Hormones; Gonadal Hormones; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists; Dibenzazepines; Heterocyclic Compounds, 3-Ring; Heterocyclic Compounds, Fused-Ring

Study Design

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

Study Record Dates

• First Submitted: October 2, 2023
• First Posted: October 6, 2023
• Study Start: January 17, 2024
• Primary Completion: April 12, 2024
• Study Completion: April 12, 2024
• Last Updated: August 12, 2025

Record last verified: 2025-08

Data Sharing

• IPD Sharing: Will share
• Time Frame: AstraZeneca will meet or exceed data availability as per the commitments made to the EFPIA/PhRMA Data-Sharing Principles. For details of our timelines, please refer to our disclosure commitment at https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure.
• Access Criteria: When a request has been approved AstraZeneca will provide access to the anonymized individual patient-level data via secure research environment Vivli.org. A Signed Data Usage Agreement (non-negotiable contract for data accessors) must be in place before accessing requested information.

Locations

US (1)