CGRP Receptor Antagonist Formulations for Healthy Subjects

Age: 18+

Sex: Any

Trial Phase: Phase 1

Sponsor: Pfizer

Must not be taking: Prescription drugs, Herbal supplements

Disqualifiers: Hematological, Renal, Endocrine, others

No Placebo Group All trial participants will receive the active study treatment (no placebo)

Compensation: Varies

Number of Visits: 1

Duration: 1 day

36 Participants Needed

What You Need to Know Before You Apply

What is the purpose of this trial?

This trial tests different versions of a medicine called a CGRP receptor antagonist to help researchers understand how these versions are absorbed and processed in the body. It targets healthy adults who meet specific criteria, such as having a body weight over 45 kg and a BMI between 16 and 32 kg/m². Participants will help determine if the different formulations of the medicine function similarly in the body. As a Phase 1 trial, the research focuses on understanding how the treatment works in people, offering participants the opportunity to be among the first to receive this new treatment.

Will I have to stop taking my current medications?

Yes, you will need to stop taking any prescription or nonprescription drugs, as well as dietary and herbal supplements, at least 14 days before the study starts.

Is there any evidence suggesting that this trial's treatments are likely to be safe?

Research has shown that the original CGRP receptor blocker, such as rimegepant, is usually well-tolerated. Studies have not identified any major safety issues, although some individuals experienced higher levels of the liver enzyme serum alanine. This increase was observed but not linked to serious health problems.

For the new version, BHV-3000, animal studies suggest safety for humans. However, past concerns about liver health with some CGRP blockers mean liver function will be closely monitored in these studies.

Both versions are being tested in healthy adults to assess absorption and processing by the body. As this trial is in an early stage, the main focus is on understanding drug metabolism and ensuring safety. ^{1 2 3 4 5}

Why are researchers excited about this trial's treatments?

Researchers are excited about CGRP receptor antagonist formulations because they represent a new way to tackle migraine prevention. Unlike traditional migraine treatments that focus on relieving symptoms after they start, CGRP receptor antagonists work by blocking the protein linked to migraine attacks before they happen. This approach not only has the potential to prevent migraines altogether but also to reduce the frequency and severity of attacks. Additionally, these formulations might offer fewer side effects compared to existing options, making them a promising alternative for many patients.

What evidence suggests that this trial's treatments could be effective?

Research has shown that CGRP receptor blockers, like the formulations studied in this trial, effectively treat migraines. These medications prevent migraines by blocking a protein called CGRP, which plays a key role in causing migraine pain. For example, atogepant, a type of CGRP blocker, reduced the frequency of migraines. Similarly, rimegepant, another CGRP blocker, effectively treats sudden migraine attacks. Both treatments are generally safe and increasingly used to prevent and relieve migraines. ^{6 7 8 9 10}

Who Is on the Research Team?

Pfizer CT.gov Call Center

Principal Investigator

Pfizer

Are You a Good Fit for This Trial?

This trial is for healthy adults over 18 years old with a BMI of 16-32 kg/m2 and weighing more than 45 kg. Participants must be able to follow the study schedule and procedures.

Inclusion Criteria

Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study

My BMI is between 16 and 32, and I weigh more than 45 kg.

I am 18 or older and considered healthy based on medical exams.

Exclusion Criteria

Any medical, psychiatric condition, suicidal ideation and behavior, laboratory abnormality or other conditions that may increase the risk of study participation or, in the investigator's judgment, make the participant inappropriate for the study

Previous administration of an investigational product (drug or vaccine) within 30 days or 5 half lives preceding the first dose of study intervention used in this study (whichever is longer). Participation in studies of other investigational products (drug or vaccine) at any time during participation in this study

A positive urine drug test. A single repeat for positive drug screen may be allowed

Timeline for a Trial Participant

Screening

Participants are screened for eligibility to participate in the trial

2-4 weeks

Treatment

Participants receive a single dose of two different formulations of a CGRP receptor antagonist to assess bioequivalence

1 day

1 visit (in-person)

Follow-up

Participants are monitored for safety and effectiveness after treatment

4 weeks

What Are the Treatments Tested in This Trial?

Interventions

• Reference formulation
• Test formulation

Trial Overview

The study compares two different formulations of a CGRP receptor antagonist medication to see if they have the same effect on the body, known as bioequivalence.

How Is the Trial Designed?

Group I: Treatment Sequence 2 Experimental Treatment 2 Interventions

Group II: Treatment Sequence 1 Experimental Treatment 2 Interventions

Who Is Running the Clinical Trial?

Pfizer

Lead Sponsor

Trials

4,712

Recruited

50,980,000+

Known For

Vaccine Innovations

Top Products

Viagra, Zoloft, Lipitor, Prevnar 13

Albert Bourla

Pfizer

Chief Executive Officer since 2019

PhD in Biotechnology of Reproduction, Aristotle University of Thessaloniki

Patrizia Cavazzoni

Pfizer

Chief Medical Officer

MD from McGill University

Citations

1.

pmc.ncbi.nlm.nih.gov

pmc.ncbi.nlm.nih.gov/articles/PMC11264921/

Efficacy and safety of atogepant, a small molecule CGRP ...

The present study aimed to systematically evaluate the efficacy and safety of atogepant, a CGRP antagonist, for migraine prophylaxis from the results of ...

2.

news.abbvie.com

news.abbvie.com/2025-12-01-AbbVie-to-Present-Phase-3-ECLIPSE-Data-Demonstrating-Atogepant-AQUIPTA-R-Superiority-Over-Placebo-in-Achieving-Pain-Freedom-for-the-Acute-Treatment-of-Migraine-at-the-19th-European-Headache-Congress

ECLIPSE trial

Atogepant is a once-daily orally administered CGRP receptor antagonist specifically developed for the preventive treatment of migraine in adults ...

3.

nejm.org

nejm.org/doi/full/10.1056/NEJMoa1811090

Rimegepant, an Oral Calcitonin Gene–Related Peptide ...

Rimegepant is an orally administered, small-molecule, calcitonin gene–related peptide receptor antagonist that may be effective in acute migraine treatment.

4.

thelancet.com

thelancet.com/journals/lancet/article/PIIS0140-6736(25)00109-6/abstract

Calcitonin gene-related peptide-targeted therapy in migraine

Small-molecule CGRP receptor antagonists called gepants have also been proven to be effective both as acute and preventive migraine treatments.

5.

mdpi.com

mdpi.com/2077-0383/10/7/1429

CGRP Receptor Antagonists and 5-HT1F Receptor Agonist ...

This review presents the data from clinical trials reporting the efficacy, safety, and tolerability of the new drugs used in the treatment of migraines.

6.

accessdata.fda.gov

accessdata.fda.gov/drugsatfda_docs/nda/2020/212728Orig1s000SumR.pdf

212728Orig1s000 SUMMARY REVIEW | FDA

Rimegepant is a calcitonin gene-related peptide. (CGRP) receptor antagonist intended for oral administration. Migraine is a primary headache ...

7.

pmc.ncbi.nlm.nih.gov

pmc.ncbi.nlm.nih.gov/articles/PMC5651004/

PMC - PubMed Central

Galcanezumab avidly binds to the human CGRP, with a binding affinity (KD) of 31 pM (4.5 ng/mL). Galcanezumab prevented the CGRP-dependent ...

8.

sciencedirect.com

sciencedirect.com/science/article/pii/S0273230019301412

Nonclinical safety evaluation of erenumab, a CGRP ...

Nonclinical data indicate no safety signal of concern for human risk. •. Nonclinical data provide adequate margins of exposure relative to the clinical dose.

9.

selleckchem.com

selleckchem.com/msds/MSDS_E7314.pdf

α-CGRP(human) | Safety Data Sheet

Safety Data Sheet · 1. Identification of substance. Product Name, α-CGRP(human). Cat. Number · 2. Composition/data on components. Chemical Name, α ...

10.

cda-amc.ca

cda-amc.ca/small-molecule-calcitonin-gene-related-peptide-receptor-antagonists-acute-treatment-migraine

Small Molecule Calcitonin Gene-Related Peptide Receptor ...

There were no safety concerns identified with these drugs in the RCTs and in a one-year extension trial; however, increases in serum alanine ...