ranolazine

Trade name: ranexa

Small moleculeapproved

Approved

Jan 27, 2006

Ranolazine is a metabolic modulator developed by Syntex (Roche) and sold under the trade name Ranexa by Gilead Sciences. Ranexa has antianginal and anti-ischemic effects that do not depend upon reductions in heart rate or blood pressure. The mechanism of action of ranolazine is unknown. It does not increase the rate-pressure product, a measure of myocardial work, at maximal exercise. In vitro studies suggest that ranolazine is a P-gp inhibitor. Ranolazine is believed to have its effects via altering the trans-cellular late sodium current. It is by altering the intracellular sodium level that ranolazine affects the sodium-dependent calcium channels during myocardial ischemia. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia. Because Ranexa prolongs the QT interval, it should be reserved for patients who have not achieved an adequate response with other antianginal drugs. Ranexa should be used in combination with amlodipine, beta-blockers or nitrates. The effect on angina rate or exercise tolerance appeared to be smaller in women than men. — NCATS

Clinical trial activity

89 trials · 74 clinical orgs · 32 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Aug 1, 2004 (NCT00091429)

Timeline

2000s

Jan 1, 2004
Gilead Sciences — Earliest Phase 3 Sponsor(trial)
Jan 27, 2006
CV Therapeutics — Earliest FDA Approval
Jan 27, 2006
CV Therapeutics — NDA Organization
Jan 27, 2006
Gilead Sciences — NDA Secondary Org
Jan 1, 2007
Earliest Phase 2 Sponsor(trial)

2010s

Jan 1, 2011
Earliest Phase 1 Sponsor(trial)
Jul 29, 2013
Lupin — Marketing Organization
May 12, 2016
Teva — Marketing Organization
Feb 27, 2017
Actavis — Marketing Organization
Dec 4, 2017
Aurobindo Pharma — Marketing Organization
May 28, 2019
Ajanta Pharma Ltd — Marketing Organization
May 28, 2019
Cipla — Marketing Organization
May 28, 2019
Sun Pharmaceuticals — Marketing Organization
May 28, 2019
Allergan PLC (2015) — Marketing Organization
Jun 4, 2019
Sciegen Pharmaceticals — Marketing Organization
Jul 5, 2019
Glenmark Pharmaceuticals — Marketing Organization
Aug 19, 2019
Zydus Discovery DMCC — Marketing Organization
Aug 19, 2019
Cadila Healthcare — Marketing Organization
Oct 29, 2019
Ani Pharmaceuticals — Marketing Organization
Oct 29, 2019
Amerigen Pharmaceuticals — Marketing Organization

2020s

Feb 12, 2020
MannKind Corp — Marketing Organization
Feb 12, 2020
Mankind Pharma — Marketing Organization
Feb 27, 2020
Micro Labs Ltd India — Marketing Organization
Mar 23, 2020
Praxgen Pharma — Marketing Organization
Mar 23, 2020
Sunshine Lake Pharma Co., Ltd. — Marketing Organization
Nov 30, 2020
Alkem Labs Ltd — Marketing Organization
Jan 28, 2021
Graviti Pharmaceuticals — Marketing Organization
Jan 28, 2021
Rising Pharmaceuticals — Marketing Organization
Mar 11, 2021
Amneal Pharmaceuticals — Marketing Organization
May 18, 2021
Accord Research — Marketing Organization
Jan 19, 2022
VKT Pharma — Marketing Organization
Feb 28, 2022
Sun Pharmaceuticals — NDA Secondary Org
Apr 27, 2022
I3 Pharms — Marketing Organization
May 5, 2022
Hetero Labs Ltd — Marketing Organization
Mar 16, 2023
Unichem — Marketing Organization
Jul 25, 2023
Piramal — Marketing Organization
Sep 27, 2023
Novast Labs — Marketing Organization

Indications

Approved for

Angina Pectoris

Studied for

Mechanism of action

Sodium channel protein type V alpha subunitBLOCKER
SCN5A blocker
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
Sodium channel protein type IV alpha subunitBLOCKER
SCN4A blocker
Competitive reversible inhibitor
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗

Approval history

approvedJan 27, 2006

Chemistry & pharmacology

Loading structure…

SMILES

COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1

Mol. weight: 427.55 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Racemic Mixture
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

Sources

Also known as

cvt-303
cvt-303
rancad
ranexa
ranexa
ranexa
ranexa
ranexa
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine
ranolazine hcl
ranolazine hydrochloride
ranolazine hydrochloride
ranolazine hydrochloride
ranolazine hydrochloride
ranolazine hydrochloride
ranolazine hydrochloride
renexa
rs-43285-003
rs-43285-003
sk-1404

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT06843044	Phase 4	Jan 13, 2025	Valenta Pharm JSC
NCT06527222	Phase 2	Dec 31, 2024	ALS Association, University of Kansas
NCT06570473	Phase 2	Dec 31, 2024	University of Alberta, University of Ottawa
NCT06012708	Phase 1	Sep 30, 2023	—
NCT05586789	Phase 3	Aug 31, 2022	Valenta Pharm JSC
NCT04456517	Phase 2	Dec 31, 2020	Vanderbilt University
NCT07054255	Phase 1	Sep 6, 2020	Haisco Pharmaceutical
NCT03401502	N/A	Jun 30, 2018	TSH Biopharm Corporation Limited
NCT03472950	Phase 2	Jun 11, 2018	Gilead Sciences, University of Kansas
NCT03486561	Phase 4	Apr 1, 2018	OBS Pakistan
NCT03162120	Phase 2/Phase 3 (Phase 3)	May 20, 2017	Aristotle University of Thessaloniki, Elpen Pharmaceutical Co. Inc.
NCT03116191	Phase 2	Feb 23, 2017	Sanwa Kagaku Kenkyusho Co., Ltd.
NCT03044964	Phase 4	Jan 10, 2017	Gilead Sciences, Stern Cardiovascular Foundation, Inc.
NCT02611596	N/A	Nov 1, 2016	United States Army
NCT03953989	Phase 2	Oct 31, 2016	Menarini Group, The Foundation Institute San Raffaele G. Giglio of Cefalù, Vita-Salute University of Milano. Italy
NCT02687269	Phase 4	Oct 1, 2016	Catholic University of Sacred Heart, Rome
NCT02878096	Phase 1	Jul 1, 2016	Quotient, Sanwa Kagaku Kenkyusho Co., Ltd.
NCT02829034	N/A	Jul 1, 2016	Gilead Sciences, Harvard University, University of Maryland, University of Pennsylvania
NCT02817932	Phase 1	Mar 1, 2016	Menarini Group, Seoul National University
NCT02252406	Phase 4	Sep 1, 2015	University of Florida

Showing 20 of 89 trials

Page 1 / 5

Organizations

Research & Development (74)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Gilead Sciences	For profit	47	18	5	2004
Harvard University	Academic/Hospital	4	1	3	2013
United States Army	Government	4	4	3	2009
Cardiovascular Institute of the South Clinical Research Corporation	Academic/Hospital	3	1	2	2009
Cedars-Sinai Medical Center	Academic/Hospital	3	2	3	2007
Menarini Group	For profit	3	2	2	2012
University of Florida	Academic/Hospital	3	1	3	2011
University of Roma La Sapienza	Academic/Hospital	3	3	1	2012
Department of Veteran Affairs	Government	2	0	1	2014
Duke University	Academic/Hospital	2	2	1	2012
Emory University	Academic/Hospital	2	1	1	2007
North Florida Foundation for Research and Education	Academic/Hospital	2	2	1	2014
Sanwa Kagaku Kenkyusho Co., Ltd.	For profit	2	2	2	2016
TSH Biopharm Corporation Limited	For profit	2	2	2	2014
University of California, San Diego	Academic/Hospital	2	2	1	2007
University of Colorado, Denver	Academic/Hospital	2	1	2	2008
University of Kansas	Academic/Hospital	2	2	1	2018
University of Maryland	Academic/Hospital	2	0	1	2013
University of Pennsylvania	Academic/Hospital	2	2	1	2013
University of Rochester	Academic/Hospital	2	2	2	2011

74 organizations

Page 1 / 4

Marketing (39)

Organization	Org type	Relationship	Date
Accord Research	For profit	MKTG	May 18, 2021
Actavis	For profit	MKTG	Feb 27, 2017
Ajanta Pharma Ltd	For profit	MKTG	May 28, 2019
Alkem Labs Ltd	For profit	MKTG	Nov 30, 2020
Allergan PLC (2015)	For profit	MKTG	May 28, 2019
Amerigen Pharmaceuticals	For profit	MKTG	Oct 29, 2019
Amneal Pharmaceuticals	For profit	MKTG	Mar 11, 2021
Ani Pharmaceuticals	For profit	MKTG	Oct 29, 2019
Ani Pharmaceuticals	For profit	MKTG	Oct 29, 2019
Aurobindo Pharma	For profit	MKTG	Dec 4, 2017
Aurobindo Pharma	For profit	SYN	Dec 23, 2022
CV Therapeutics	For profit	NDA	Jan 27, 2006
Cadila Healthcare	For profit	MKTG	Aug 19, 2019
Cipla	For profit	MKTG	May 28, 2019
Gilead Sciences	For profit	NDA2	Jan 27, 2006
Glenmark Pharmaceuticals	For profit	MKTG	Jul 5, 2019
Graviti Pharmaceuticals	For profit	MKTG	Jan 28, 2021
Hetero Labs Ltd	For profit	MKTG	May 5, 2022
I3 Pharms	For profit	MKTG	Apr 27, 2022
Lupin	For profit	MKTG	Jul 29, 2013
Mankind Pharma	For profit	MKTG	Feb 12, 2020
MannKind Corp	For profit	MKTG	Feb 12, 2020
Micro Labs Ltd India	For profit	MKTG	Feb 27, 2020
Novast Labs	For profit	MKTG	Sep 27, 2023
Novast Labs	For profit	SYN	Sep 27, 2023
Piramal	For profit	MKTG	Jul 25, 2023
Praxgen Pharma	For profit	MKTG	Mar 23, 2020
Praxgen Pharma	For profit	SYN	Mar 23, 2020
Rising Pharmaceuticals	For profit	MKTG	Jan 28, 2021
Sciegen Pharmaceticals	For profit	MKTG	Jun 4, 2019
Sun Pharmaceuticals	For profit	SYN	Feb 28, 2022
Sun Pharmaceuticals	For profit	MKTG	May 28, 2019
Sun Pharmaceuticals	For profit	NDA2	Feb 28, 2022
Sunshine Lake Pharma Co., Ltd.	For profit	MKTG	Mar 23, 2020
Sunshine Lake Pharma Co., Ltd.	For profit	SYN	Mar 23, 2020
Teva	For profit	MKTG	May 12, 2016
Unichem	For profit	MKTG	Mar 16, 2023
VKT Pharma	For profit	MKTG	Jan 19, 2022
Zydus Discovery DMCC	For profit	MKTG	Aug 19, 2019