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Gefapixant

Generic Name
Gefapixant
Brand Names
Lyfnua
Drug Type
Small Molecule
Chemical Formula
C14H19N5O4S
CAS Number
1015787-98-0
Unique Ingredient Identifier
6K6L7E3F1L
Background

It has been estimated that 5-10% of adults globally suffer from chronic cough, which is defined as a cough lasting longer than eight weeks. A subset of these patients remain symptomatic despite thorough investigation and treatment, termed refractory chronic cough (RCC) if they have a cough that does not respond to conventional treatment or unexplained chronic cough (UCC) when no diagnosable cause for the cough can be determined. Existing treatments for chronic cough have been associated with considerable side effects, in particular opioids such as codeine or dextromethorphan.

Gefapixant is a novel antagonist of the P2X3 receptor that works to reduce the cough reflex in patients with chronic cough. It received approval in both Japan and Switzerland in 2022 for the treatment of adult patients with RCC and UCC, and received subsequent approval in the EU in September 2023 for the same indications. It is the first therapy to be approved for the treatment of RCC or UCC in the EU.

Indication

用于成人治疗难治性慢性咳嗽(RCC)或不明原因慢性咳嗽(UCC)。

Associated Conditions
Refractory Chronic Cough, Unexplained Chronic Cough

A Study of Gefapixant (MK-7264) in Adult Participants With Chronic Cough (MK-7264-027)

Phase 3
Completed
Conditions
Chronic Cough
Interventions
Drug: Placebo
First Posted Date
2018-02-28
Last Posted Date
2021-06-16
Lead Sponsor
Merck Sharp & Dohme LLC
Target Recruit Count
732
Registration Number
NCT03449134
Locations
🇺🇸

Research Solutions of Arizona PC ( Site 0036), Litchfield Park, Arizona, United States

🇺🇸

Medical Research of AZ ( Site 0060), Scottsdale, Arizona, United States

🇦🇷

InAER Investigaciones en Alergia y Enfermedades Respiratorias ( Site 0324), Caba, Buenos Aires, Argentina

and more 153 locations

A Study of Gefapixant (MK-7264) in Adult Participants With Chronic Cough (MK-7264-030)

Phase 3
Completed
Conditions
Chronic Cough
Interventions
First Posted Date
2018-02-28
Last Posted Date
2021-09-02
Lead Sponsor
Merck Sharp & Dohme LLC
Target Recruit Count
1317
Registration Number
NCT03449147
Locations
🇺🇸

Bethesda Allergy Asthma and Research Center LLC ( Site 0019), Bethesda, Maryland, United States

🇺🇸

Atlanta Allergy & Asthma Clinic PA ( Site 0029), Stockbridge, Georgia, United States

🇺🇸

University of Missouri ENT & Allergy Center ( Site 0066), Columbia, Missouri, United States

and more 168 locations

The Pharmacokinetics of Gefapixant (MK-7264) in Participants With Renal Insufficiency (MK-7264-026)

Phase 1
Completed
Conditions
Renal Insufficiency
Interventions
First Posted Date
2017-04-11
Last Posted Date
2022-07-27
Lead Sponsor
Merck Sharp & Dohme LLC
Target Recruit Count
24
Registration Number
NCT03108924
Locations
🇺🇸

Clinical Pharmacology of Miami ( Site 0001), Hialeah, Florida, United States

🇺🇸

Orlando Clinical Research Center ( Site 0002), Orlando, Florida, United States

A Multiple-Dose Pharmacokinetics Study of Three Gefapixant (AF-219/MK-7264) Formulations

Phase 1
Completed
Conditions
Healthy
Interventions
First Posted Date
2016-06-06
Last Posted Date
2017-04-18
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
32
Registration Number
NCT02790840
Locations
🇺🇸

Celerion, Tempe, Arizona, United States

A 12-Week Study in Participants With Refractory Chronic Cough (MK-7264-012)

Phase 2
Completed
Conditions
Refractory Chronic Cough
Interventions
Drug: Placebo (for gefapixant)
First Posted Date
2015-11-24
Last Posted Date
2020-06-30
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
253
Registration Number
NCT02612610

An 8-Week Refractory Chronic Cough Study (MK-7264-021)

Phase 2
Completed
Conditions
Refractory Chronic Cough
Interventions
Drug: Placebo (for gefapixant)
First Posted Date
2015-11-24
Last Posted Date
2019-11-25
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
24
Registration Number
NCT02612623
Locations
🇺🇸

Afferent Investigative Site, Greenfield, Wisconsin, United States

A Study of Gefapixant (AF-219/MK-7264) in Participants With Idiopathic Pulmonary Fibrosis (IPF) With Persistent Cough (MK-7264-016)

Phase 2
Completed
Conditions
Idiopathic Pulmonary Fibrosis
Cough
Interventions
Other: Placebo
First Posted Date
2015-07-20
Last Posted Date
2021-05-26
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
51
Registration Number
NCT02502097

A Multiple-Dose Pharmacokinetics Study of Two Gefapixant (AF-219/MK-7264) Formulations

Phase 1
Completed
Conditions
Healthy
Interventions
First Posted Date
2015-07-09
Last Posted Date
2022-07-22
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
14
Registration Number
NCT02492776
Locations
🇺🇸

Celerion, Tempe, Arizona, United States

A Study to Assess the Tolerability of a Single Dose of Gefapixant (AF-219/MK-7264) in Subjects With Idiopathic Pulmonary Fibrosis (IPF)

Phase 2
Completed
Conditions
Idiopathic Pulmonary Fibrosis
Interventions
First Posted Date
2015-06-23
Last Posted Date
2019-06-25
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
6
Registration Number
NCT02477709
Locations
🇺🇸

American Health Research, Charlotte, North Carolina, United States

Effect of Gefapixant (MK-7264/AF-219) on Cough Reflex Sensitivity in Healthy and Chronic Cough Participants (MK-7264-014)

Phase 2
Completed
Conditions
Refractory Chronic Cough
Interventions
First Posted Date
2015-06-22
Last Posted Date
2019-06-18
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
36
Registration Number
NCT02476890
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