revefenacin

Trade name: yupelri

Small moleculeapproved

Approved

Nov 9, 2018

Revefenacin (trade name Yupelri is a long-acting muscarinic antagonist developed by Mylan Ireland ltd for the treatment of chronic obstructive pulmonary disease (COPD). It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo models, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. — NCATS

Clinical trial activity

19 trials · 5 clinical orgs · 3 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Dec 1, 2007 (NCT00555022)

Timeline

2000s

Jan 1, 2007
Earliest Phase 1 Sponsor(trial)

2010s

Jan 1, 2011
Theravance — Earliest Phase 2 Sponsor(trial)
Jan 1, 2015
Theravance — Earliest Phase 3 Sponsor(trial)
Nov 9, 2018
Theravance — Earliest FDA Approval
Nov 9, 2018
Mylan — NDA Secondary Org
Nov 9, 2018
Theravance — NDA Organization

2020s

Jan 6, 2025
Mankind Pharma — Marketing Organization

Indications

Approved for

Pulmonary Disease, Chronic Obstructive (approved 2018)

Studied for

Mechanism of action

Muscarinic acetylcholine receptorANTAGONIST
Muscarinic acetylcholine receptor antagonist
Muscarinic acetylcholine receptor M3ANTAGONIST
Muscarinic acetylcholine receptor M3 antagonist
Inhibits the muscarinic M3 receptor leading to bronchodilation.
Similar affinity for muscarinic receptors M1-M5 but bronchodilation mediated via receptor M3.
- Muscarinic acetylcholine receptor M3 (CHRM3) ↗

Approval history

approvedNov 9, 2018

Chemistry & pharmacology

Loading structure…

SMILES

CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CN2CCC(C(N)=O)CC2)cc1

Mol. weight: 597.76 g/mol
Lipinski Ro5: 1 violation(s)
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Topical
Availability: Prescription Only

Oral

Parenteral

Topical

Yes

Sources

Also known as

biphenyl-2-ylcarbamic acid 1-(2-((4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl)methylamino)ethyl)piperidin-4-yl ester
gsk1160724
gsk1160724
revefenacin
revefenacin
revefenacin
revefenacin
td-4208
td-4208
td-4208

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT05165485	Phase 4	Dec 31, 2021	Mylan, Theravance
NCT05207111	Phase 1	Sep 23, 2021	Mylan
NCT05046795	Phase 3	Sep 15, 2021	Mylan
NCT04655170	Phase 4	Dec 20, 2020	Mylan, University of Tennessee
NCT04315558	Phase 2	Apr 30, 2020	Mylan, Theravance, University of California, Los Angeles
NCT03573817	Phase 3	May 31, 2018	Mylan, Theravance
NCT03095456	Phase 3	Mar 20, 2017	Theravance
NCT02820311	Phase 1	May 1, 2016	Theravance
NCT02578082	Phase 1/Phase 2 (Phase 2)	Dec 1, 2015	Theravance
NCT02581592	Phase 1/Phase 2 (Phase 2)	Nov 1, 2015	Theravance
NCT02518139	Phase 3	Sep 1, 2015	Theravance
NCT02512510	Phase 3	Sep 1, 2015	Theravance
NCT02459080	Phase 3	Sep 1, 2015	Theravance
NCT02772159	Phase 1	Jun 1, 2015	Theravance
NCT02040792	Phase 2	May 1, 2014	Theravance
NCT02109172	Phase 2	Apr 1, 2014	Theravance
NCT01704404	Phase 2	Dec 1, 2012	Theravance
NCT03064113	Phase 2	May 1, 2011	Theravance
NCT00555022	Phase 1	Dec 1, 2007	GlaxoSmithKline

Showing 19 of 19 trials

Page 1 / 1

Organizations

Research & Development (5)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Theravance	For profit	15	14	4	2011
Mylan	For profit	6	2	4	2018
GlaxoSmithKline	For profit	1	1	1	2007
University of California, Los Angeles	Academic/Hospital	1	1	1	2020
University of Tennessee	Academic/Hospital	1	1	1	2020

5 organizations

Page 1 / 1

Marketing (3)

Organization	Org type	Relationship	Date
Mankind Pharma	For profit	MKTG	Jan 6, 2025
Mylan	For profit	NDA2	Nov 9, 2018
Theravance	For profit	NDA	Nov 9, 2018