naltrexone

Trade name: revia

Small moleculeapproved

Approved

Dec 7, 1953

Naltrexone is marketed as its hydrochloride salt, naltrexone hydrochloride, under the trade names Revia and Depade. A once-monthly extended-release injectable formulation is marketed under the trade name Vivitrol. VIVITROL is indicated for the treatment of alcohol dependence in patients who are able to abstain from alcohol in an outpatient setting prior to initiation of treatment with VIVITROL. VIVITROL is indicated for the prevention of relapse to opioid dependence, following opioid detoxification. Naltrexone is a pure opiate antagonist and has little or no agonist activity. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone is thought to act as a competitive antagonist at mc, κ, and δ receptors in the CNS, with the highest affinity for the μ receptor. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. This leads to the antagonization of most of the subjective and objective effects of opiates, including respiratory depression, miosis, euphoria, and drug craving. The major metabolite of naltrexone, 6-β-naltrexol, is also an opiate antagonist and may contribute to the antagonistic activity of the drug. Low dose naltrexone is an “off label” use of naltrexone. Normal naltrexone usage to break addictions is 50mg – 100mg. Usage of low dose naltrexone ranges in the area of 3 mg – 4.5 mg dosing and is prescribed in an oral pill form and is quite inexpensive. For people with multiple sclerosis, the dosage of LDN ranges from 1.5 to 4.5 ml per day. — NCATS

Clinical trial activity

1,500 trials · 781 clinical orgs · 56 marketing orgs

Phase 1

205

Phase 2

957

Phase 3

422

Phase 4

238

Earliest trial started May 1, 1986 (NCT00002456)

Timeline

1950s

Dec 7, 1953
Earliest FDA Approval
Dec 7, 1953
DAVA Pharmaceuticals — NDA Secondary Org
Dec 7, 1953
Strides Pharma Science — Marketing Organization
Dec 7, 1953
Strides Pharma Science — NDA Secondary Org
Aug 10, 1959
Hospira — NDA Secondary Org

1970s

Sep 5, 1979
Bristol-Myers — Marketing Organization

1980s

Nov 20, 1984
DuPont — First NDA Organization
Nov 20, 1984
DuPont — NDA Organization
Nov 20, 1984
Teva — NDA Secondary Org
Jan 1, 1986
Earliest Phase 3 Sponsor(trial)
May 9, 1986
Norbrook — Marketing Organization
Jun 13, 1986
Abraxis — Marketing Organization
Sep 16, 1986
West-Ward Pharmaceutical — Marketing Organization
Jan 1, 1987
Earliest Phase 2 Sponsor(trial)
Apr 14, 1989
Bristol-Myers Squibb — Marketing Organization

1990s

Oct 15, 1990
Barr Laboratories — Marketing Organization
Aug 23, 1991
Pharmacia & Upjohn — Marketing Organization
May 15, 1992
Mylan — Marketing Organization
Jan 1, 1994
Earliest Phase 1 Sponsor(trial)
Aug 1, 1994
Hikma — Marketing Organization
Feb 26, 1999
Fresenius — Marketing Organization
May 26, 1999
Elite Laboratories, Inc — Marketing Organization
Jun 17, 1999
Duramed Research — Marketing Organization

2000s

Mar 8, 2000
Fosun — Marketing Organization
Mar 22, 2002
Specgx Llc — Marketing Organization
Apr 13, 2006
Alkermes — NDA Secondary Org
Apr 30, 2007
Accord Research — Marketing Organization
Mar 31, 2009
Sandoz — Marketing Organization
Mar 31, 2009
Novartis — Marketing Organization
Aug 13, 2009
Alpharma — Marketing Organization
Aug 13, 2009
King Pharmaceuticals — NDA Secondary Org

2010s

Jan 8, 2010
Pharmachemie Bv — Marketing Organization
Jan 8, 2010
Teva — Marketing Organization
Feb 24, 2012
Sun Pharmaceuticals — Marketing Organization
Mar 29, 2012
Rising Pharmaceuticals — Marketing Organization
Mar 29, 2012
EXTROVIS — Marketing Organization
Oct 11, 2013
Antares Pharma Inc. — NDA Secondary Org
Oct 11, 2013
Assertio — NDA Secondary Org
Jul 10, 2014
Medac — NDA Secondary Org
Jul 10, 2014
MEDEX — Marketing Organization
Jul 10, 2014
Smiths Medical, ASD, Inc. — NDA Secondary Org
Sep 10, 2014
Nalpropion — Marketing Organization
Sep 10, 2014
Nalpropion — NDA Secondary Org
Aug 19, 2016
Pfizer — Marketing Organization
Aug 19, 2016
Pfizer — NDA Secondary Org
Jan 13, 2017
Zydus Discovery DMCC — Marketing Organization
Apr 25, 2017
Silvergate Pharmaceuticals — NDA Secondary Org
Apr 25, 2017
Azurity — Marketing Organization
Apr 25, 2017
Azurity — NDA Secondary Org
Jul 21, 2017
Apotex — Marketing Organization
Jul 21, 2017
Chartwell Pharmaceuticals — Marketing Organization
Dec 22, 2017
Amneal Pharmaceuticals — Marketing Organization
Aug 9, 2018
Sagent Pharmaceuticals, Inc. — Marketing Organization
Aug 9, 2018
Nichi-Iko Pharmaceutical Co., Ltd. — Marketing Organization
Nov 27, 2019
Cumberland Pharmaceuticals — Marketing Organization
Nov 27, 2019
Nordic Group BV — NDA Secondary Org

2020s

Jan 30, 2020
Eugia Pharma — Marketing Organization
Aug 24, 2020
Accord Research — NDA Secondary Org
Apr 23, 2021
Lotus Pharmaceutical — Marketing Organization
Apr 23, 2021
Alvogen — Marketing Organization
Nov 29, 2022
AbbVie — Marketing Organization
Nov 29, 2022
Therakind Ltd — NDA Secondary Org
Nov 29, 2022
SHORLA — Marketing Organization
Aug 7, 2023
Daito Pharmaceuticals — Marketing Organization
Jun 3, 2024
Alembic — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Opioid receptors; mu/kappa/deltaANTAGONIST
Opioid receptors; mu/kappa/delta antagonist
Dihydrofolate reductaseINHIBITOR
DHFR inhibitor
- Dihydrofolate reductase (DHFR) ↗

Combination products

contrave
with bupropion
embeda
with morphine
troxyca er
with oxycodone

Approval history

approvedPriority reviewDec 7, 1953

Chemistry & pharmacology

Loading structure…

SMILES

OC1=C2O[C@H]3C(=O)CC[C@@]4(O)[C@H]5CC(C=C1)=C2[C@@]34CCN5CC6CC6

Mol. weight: 341.4009 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

Black box warning

Sources

Also known as

17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6-one
17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6-one
4-amino-10-methylfolic acid
4-amino-10-methylfolic acid
4-amino-n(10)-methylpteroylglutamic acid
4-amino-n(10)-methylpteroylglutamic acid
abitrexate
abitrexate
abitrexate
adepend
amethopterin
amethopterin
amethopterin
amethopterin
amethopterin
amethopterine
atnc05
bupropion hydrochloride / naltrexone hydrochloride
celupan
celupan
cl-14377
cl-14377
cl-14377
cyclopropylmethylnoroxymorphone
depade
depade
ebetrex
emtexate high-pot
emtexate pf
en-1639a
en-1639a
en-1639a [as hydrochloride]
en-1639a [as hydrochloride]
folex
folex
folex
folex
folex pfs
folex pfs
folex pfs
l-amethopterin
ledertrexate
ledertrexate
maxtrex
maxtrex
maxtrex
merphos
metatrexan
methotrexat
methotrexat
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
methotrexate
méthotrexate
méthotrexate
methotrexate lpf
methotrexate lpf
methotrexate lpf
methotrexate sodium
methotrexate sodium
methotrexate sodium
methotrexate sodium
methotrexatum
methotrexatum
methotrexatum
methoxtrexate
methrexate
methylaminopterin
methylaminopterin
methylaminopterin
metoject
metotrexato
metotrexato
metotrexato
mexate
mexate
mexate
mexate
mexate-aq
mexate-aq
mexate-aq
mexate-aq preserved
mexate-aq preserved
mtx
mtx
mtx
n-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-l-glutamic acid
n-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-l-glutamic acid
nalorex
nalorex
naltrel
naltrexon
naltrexon
naltrexona
naltrexona
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone
naltrexone hcl
naltrexone hcl
naltrexone hcl
naltrexone-hcl
naltrexone hydrochloride
naltrexone hydrochloride
naltrexone hydrochloride
naltrexone hydrochloride
naltrexone hydrochloride dihydrate
naltrexonum
naltrexonum
natrexone
natrexone
n-cyclopropylmethyl-14-hydroxydihydromorphinone
n-cyclopropylmethyl-14-hydroxydihydromorphinone
n-cyclopropylmethylnoroxymorphone
n-cyclopropylmethylnoroxymorphone
opizone
phosphorotrithious acid, tributyl ester
revia
revia
revia
rheumatrex
rheumatrex
rheumatrex
s,s,s-tributyl phosphorotrithioite
tcmdc-123832
tcmdc-123832
tcmdc-125488
tcmdc-125488
tcmdc-125858
tcmdc-125858
trexal
trexall
trexall
trexan
trexan
trexan
vivitrol
vivitrol
vivitrol
zlatal

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT07285473	Phase 2	Apr 1, 2026	University of Alabama, Birmingham
NCT07249554	Phase 2	Mar 31, 2026	Johns Hopkins University
NCT07064564	Phase 1	Feb 1, 2026	Albert Einstein Israelite Hospital, Ardena, CenExel iResearch, LLC, Drug Delivery International Ltd, National Institute on Drug Abuse (NIDA)
NCT07224009	Phase 2	Jan 31, 2026	University of Arkansas
NCT07269873	Phase 1	Jan 13, 2026	BioCorRx Pharmaceuticals, Inc., National Institute on Drug Abuse (NIDA)
NCT07224087	Phase 1	Jan 1, 2026	Yale University
NCT07213466	Phase 4	Dec 1, 2025	Mayo Clinic, University of Toronto
NCT07132177	Phase 2	Nov 3, 2025	Harvard University
NCT07221565	Phase 1/Phase 2 (Phase 2)	Oct 23, 2025	Truway Health, Inc.
NCT06845124	Phase 2	Jul 1, 2025	German Federal Ministry of Education and Research, Heidelberg University, University of Heidelberg
NCT06845345	Phase 4	Apr 14, 2025	Franciscus Gasthuis
NCT06854614	Phase 4	Mar 1, 2025	The Cleveland Clinic
NCT06723561	Phase 2	Jan 1, 2025	Medical College of Wisconsin
NCT07092618	Phase 2/Phase 3 (Phase 3)	Dec 17, 2024	AgelessRx
NCT06633900	Phase 2/Phase 3 (Phase 3)	Dec 15, 2024	National Institute on Drug Abuse (NIDA), University of California, San Francisco
NCT06622239	Phase 2	Dec 1, 2024	Seoul National University, Whanin Pharmaceutical Company
NCT06306157	Phase 4	Oct 31, 2024	Rockefeller University
NCT06620562	Phase 4	Oct 15, 2024	Laval University
NCT06605703	Phase 4	Sep 18, 2024	Weight Watchers International
NCT06366724	Phase 2	Aug 31, 2024	Harvard University

Showing 20 of 1,500 trials

Page 1 / 75

Organizations

Research & Development (781)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
National Cancer Institute (NCI)	Government	249	102	5	1987
National Institute on Drug Abuse (NIDA)	Government	77	8	5	1993
Roche	For profit	61	47	5	2001
University of Texas at Houston	Academic/Hospital	55	53	5	1989
National Institute on Alcohol Abuse and Alcoholism (NIAAA)	Government	50	9	5	1992
Harvard University	Academic/Hospital	47	40	5	1999
University of Washington	Academic/Hospital	45	43	5	1986
University of Pennsylvania	Academic/Hospital	42	34	5	1995
Pfizer	For profit	41	34	4	2002
Yale University	Academic/Hospital	39	36	5	1993
Columbia University	Academic/Hospital	33	20	5	1996
University of California, San Francisco	Academic/Hospital	33	21	5	1996
St. Jude Children's Hospital	Academic/Hospital	27	25	4	1993
Genentech	For profit	25	16	5	2002
Alkermes	For profit	24	13	3	2002
Amgen	For profit	22	10	5	1999
Cornell University	Academic/Hospital	22	20	5	1990
Department of Veteran Affairs	Government	22	11	4	1993
University of Minnesota	Academic/Hospital	20	16	5	1996
University of Southern California	Academic/Hospital	20	14	4	1997

781 organizations

Page 1 / 40

Marketing (73)

Organization	Org type	Relationship	Date
AbbVie	For profit	MKTG	Nov 29, 2022
Abic	For profit	MKTG	—
Abraxis	For profit	MKTG	Jun 13, 1986
Accord Research	For profit	MKTG	Apr 30, 2007
Accord Research	For profit	SYN	Aug 24, 2020
Accord Research	For profit	NDA2	Aug 24, 2020
Alembic	For profit	MKTG	Jun 3, 2024
Alkermes	For profit	NDA2	Apr 13, 2006
Alpharma	For profit	MKTG	Aug 13, 2009
Alvogen	For profit	MKTG	Apr 23, 2021
Amneal Pharmaceuticals	For profit	MKTG	Dec 22, 2017
Antares Pharma Inc.	For profit	NDA2	Oct 11, 2013
Apotex	For profit	MKTG	Jul 21, 2017
Apotex	For profit	SYN	Jul 21, 2017
Assertio	For profit	NDA2	Oct 11, 2013
Athenex, Inc.	For profit	MKTG	—
Azurity	For profit	MKTG	Apr 25, 2017
Azurity	For profit	NDA2	Apr 25, 2017
Barr Laboratories	For profit	MKTG	Oct 15, 1990
Bristol-Myers	For profit	MKTG	Sep 5, 1979
Bristol-Myers Squibb	For profit	SYN	Feb 14, 1985
Bristol-Myers Squibb	For profit	MKTG	Apr 14, 1989
Chartwell Pharmaceuticals	For profit	MKTG	Jul 21, 2017
Cumberland Pharmaceuticals	For profit	MKTG	Nov 27, 2019
DAVA Pharmaceuticals	For profit	NDA2	Dec 7, 1953
Daito Pharmaceuticals	For profit	MKTG	Aug 7, 2023
DuPont	For profit	NDA	Nov 20, 1984
Duramed Research	For profit	MKTG	Jun 17, 1999
EXTROVIS	For profit	MKTG	Mar 29, 2012
Elite Laboratories, Inc	For profit	SYN	May 16, 2024
Elite Laboratories, Inc	For profit	MKTG	May 26, 1999
Eugia Pharma	For profit	MKTG	Jan 30, 2020
Eugia Pharma	For profit	SYN	Mar 29, 2012
Fosun	For profit	MKTG	Mar 8, 2000
Fresenius	For profit	MKTG	Feb 26, 1999
Hikma	For profit	MKTG	Aug 1, 1994
Hikma	For profit	SYN	Sep 16, 1986
Hospira	For profit	NDA2	Aug 10, 1959
King Pharmaceuticals	For profit	NDA2	Aug 13, 2009
Lotus Pharmaceutical	For profit	MKTG	Apr 23, 2021
MEDEX	For profit	MKTG	Jul 10, 2014
Medac	For profit	NDA2	Jul 10, 2014
Mylan	For profit	MKTG	May 15, 1992
Mylan	For profit	SYN	Mar 29, 2012
Nalpropion	For profit	MKTG	Sep 10, 2014
Nalpropion	For profit	NDA2	Sep 10, 2014
Nichi-Iko Pharmaceutical Co., Ltd.	For profit	MKTG	Aug 9, 2018
Norbrook	For profit	MKTG	May 9, 1986
Nordic Group BV	For profit	NDA2	Nov 27, 2019
Novartis	For profit	MKTG	Mar 31, 2009
Pfizer	For profit	MKTG	Aug 19, 2016
Pfizer	For profit	NDA2	Aug 19, 2016
Pharmachemie Bv	For profit	MKTG	Jan 8, 2010
Pharmachemie Bv	For profit	SYN	Jul 8, 1988
Pharmacia & Upjohn	For profit	MKTG	Aug 23, 1991
Rising Pharmaceuticals	For profit	MKTG	Mar 29, 2012
SHORLA	For profit	MKTG	Nov 29, 2022
Sagent Pharmaceuticals, Inc.	For profit	MKTG	Aug 9, 2018
Sagent Pharmaceuticals, Inc.	For profit	SYN	Aug 9, 2018
Sandoz	For profit	MKTG	Mar 31, 2009
Silvergate Pharmaceuticals	For profit	NDA2	Apr 25, 2017
Smiths Medical, ASD, Inc.	For profit	NDA2	Jul 10, 2014
Specgx Llc	For profit	MKTG	Mar 22, 2002
Strides Pharma Science	For profit	MKTG	Dec 7, 1953
Strides Pharma Science	For profit	NDA2	Dec 7, 1953
Sun Pharmaceuticals	For profit	SYN	Feb 24, 2012
Sun Pharmaceuticals	For profit	MKTG	Feb 24, 2012
Teva	For profit	NDA2	Nov 20, 1984
Teva	For profit	MKTG	Jan 8, 2010
Teva	For profit	SYN	Jul 6, 2023
Therakind Ltd	For profit	NDA2	Nov 29, 2022
West-Ward Pharmaceutical	For profit	MKTG	Sep 16, 1986
Zydus Discovery DMCC	For profit	MKTG	Jan 13, 2017