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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

Effect of Gefapixant (AF-219/MK-7264) on Cough Reflex Sensitivity (MK-7264-015)

Phase 2
Completed
Conditions
Refractory Chronic Cough
Interventions
Drug: Placebo
First Posted Date
2015-03-25
Last Posted Date
2021-02-12
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
50
Registration Number
NCT02397460
Locations
🇬🇧

The Medicines Evaluation Unit, Manchester, United Kingdom

A Dose Escalation Study of Gefapixant (AF-219/MK-7264) in Refractory Chronic Cough (MK-7264-010)

Phase 2
Completed
Conditions
Refractory Chronic Cough
Interventions
Drug: Placebo (for gefapixant)
First Posted Date
2015-01-28
Last Posted Date
2020-10-22
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
59
Registration Number
NCT02349425

A Study to Assess the Effect of Intragastric pH and Fasting on the Pharmacokinetics of Gefapixant (AF-219/MK-7264)

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
First Posted Date
2014-09-03
Last Posted Date
2022-07-22
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
18
Registration Number
NCT02229877

A Study to Evaluate the Effect of Gefapixant (AF-219/MK-7264) on Methacholine Hyper-reactivity in Participants With Asthma (MK-7264-009)

Phase 2
Completed
Conditions
Asthma
Interventions
Drug: Placebo to mimic 50 mg tablets
Drug: Placebo to mimic 300 mg tablets
First Posted Date
2013-11-25
Last Posted Date
2021-02-03
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
20
Registration Number
NCT01993329

The Safety and Efficacy of Gefapixant (AF-219/MK-7264) in Female Participants With Interstitial Cystitis /Bladder Pain Syndrome (MK-7264-005)

Phase 2
Terminated
Conditions
Bladder Pain Syndrome
Interventions
Drug: Placebo
First Posted Date
2012-04-03
Last Posted Date
2020-08-17
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
107
Registration Number
NCT01569438
Locations
🇺🇸

Afferent Investigative Site, Virginia Beach, Virginia, United States

A Four-Week Multicenter Study Evaluating the Safety and Efficacy of Gefapixant (AF-219/MK-7264) in Subjects With Osteoarthritis of the Knee

Phase 2
Completed
Conditions
Osteoarthritis of the Knee
Interventions
Drug: Sugar Pill
First Posted Date
2012-03-15
Last Posted Date
2019-06-27
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
171
Registration Number
NCT01554579
Locations
🇺🇸

Afferent Investigative Site, Kenosha, Wisconsin, United States

A Study to Assess the Efficacy of Gefapixant (MK-7264/AF-219), in Participants With Chronic Cough (MK-7264-006)

Phase 2
Completed
Conditions
Chronic Cough
Interventions
Drug: Placebo
First Posted Date
2011-09-13
Last Posted Date
2020-11-24
Lead Sponsor
Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Target Recruit Count
24
Registration Number
NCT01432730
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