buprenorphine

Small moleculeapproved

Approved

Dec 29, 1981

Buprenorphine is an opioid analgesic, used to treat opioid addiction, moderate acute pain, and moderate chronic pain. Buprenorphine is a partial agonist at the mµ-opioid receptor and an antagonist at the kappa-opioid receptor. One unusual property of buprenorphine observed in vitro studies is its very slow rate of dissociation from its receptor. This could account for its longer duration of action than morphine, the unpredictability of its reversal by opioid antagonists, and its low level of manifest physical dependence. The principal action of the therapeutic value of buprenorphine is analgesia and is thought to be due to buprenorphine binding with high affinity to opioid receptors on neurons in the brain and spinal cord. Buprenorphine produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Buprenorphine causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Buprenorphine produces peripheral vasodilation, which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension. — NCATS

Clinical trial activity

457 trials · 265 clinical orgs · 36 marketing orgs

Phase 1

Phase 2

226

Phase 3

120

Phase 4

103

Earliest trial started Aug 1, 1988 (NCT00000204)

Timeline

1980s

Dec 29, 1981
Indivior Inc. — Earliest FDA Approval
Dec 29, 1981
Indivior Inc. — NDA Secondary Org
Dec 29, 1981
Norwich Eaton Company — NDA Secondary Org
Dec 29, 1981
Indivior Inc. — NDA Organization
Jan 1, 1988
Earliest Phase 2 Sponsor(trial)

1990s

Jan 1, 1990
Earliest Phase 3 Sponsor(trial)
Jan 1, 1991
Earliest Phase 1 Sponsor(trial)
Jun 3, 1996
Hospira — Marketing Organization

2000s

Mar 2, 2005
West-Ward Pharmaceutical — Marketing Organization
Mar 27, 2007
Lutipold — Marketing Organization
Mar 27, 2007
Sankyo — Marketing Organization
Mar 27, 2007
Daiichi Sankyo — Marketing Organization
Oct 8, 2009
Hikma — Marketing Organization

2010s

May 7, 2010
Barr Laboratories — Marketing Organization
Jun 30, 2010
Purdue Pharmaceuticals — NDA Secondary Org
Sep 24, 2010
Ethypharm — Marketing Organization
Feb 22, 2013
Actavis — Marketing Organization
Feb 22, 2013
Amneal Pharmaceuticals — Marketing Organization
Jul 3, 2013
Orexo AB — Marketing Organization
Jul 3, 2013
Orexo AB — NDA Secondary Org
Jun 6, 2014
BioDelivery Sciences International — NDA Secondary Org
Jun 10, 2015
CASI Pharmaceuticals, Inc. — Marketing Organization
Jun 10, 2015
Rubicon Research — Marketing Organization
Jul 28, 2015
Par Pharmaceuticals — Marketing Organization
Jul 28, 2015
Bristol-Myers Squibb — Marketing Organization
Jan 29, 2016
Sun Pharmaceuticals — Marketing Organization
May 26, 2016
Titan Pharmaceuticals — NDA Secondary Org
Sep 19, 2016
Lannett Company, Inc. — Marketing Organization
Mar 27, 2017
Rhodes Pharmaceuticals, L.P. — Marketing Organization
Oct 24, 2017
Allergan PLC (2015) — Marketing Organization
Dec 13, 2017
Specgx Llc — Marketing Organization
Dec 13, 2017
Mallinckrodt (2013) — Marketing Organization
Jun 14, 2018
Dr. Reddy's Laboratories — Marketing Organization
Sep 7, 2018
Teva — NDA Secondary Org
Nov 20, 2018
Teva — Marketing Organization
Dec 21, 2018
Braeburn Pharmaceuticals — NDA Secondary Org
Jan 24, 2019
Alvogen — Marketing Organization

2020s

Jul 17, 2020
Mayne Pharma — Marketing Organization
Jul 17, 2020
Wes Pharma Inc — Marketing Organization
May 3, 2021
Mylan — Marketing Organization
Jun 15, 2021
Alkem Labs Ltd — Marketing Organization
Sep 23, 2021
Aveva Drug Delivery Systems — Marketing Organization
Sep 23, 2021
Apotex — Marketing Organization
May 23, 2023
Braeburn Pharmaceuticals — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Kappa opioid receptorAGONIST
OPRK1 agonist
- Kappa-type opioid receptor (OPRK1) ↗
Mu opioid receptorAGONIST
OPRM agonist
- Mu-type opioid receptor (OPRM) ↗

Combination products

suboxone
with naloxone
Also known as bunavail, cassipa, zubsolv

Approval history

approvedDec 29, 1981

Chemistry & pharmacology

Loading structure…

SMILES

CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5

Mol. weight: 467.65 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Parenteral, Topical
Availability: Prescription Only

Oral

Parenteral

Yes

Topical

Yes

Black box warning

Sources

Also known as

17-cyclopropylmethyl-4,5alpha-epoxy-7alpha-((s)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol
17-cyclopropylmethyl-4,5alpha-epoxy-7alpha-((s)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol
21-cyclopropyl-7alpha-[(s)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine
21-cyclopropyl-7alpha-[(s)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine
2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(14r)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-3,3-dimethyl-2-butanol
2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(14r)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-3,3-dimethyl-2-butanol
2-(n-cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol
2-(n-cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol
bupeaze
buplast
buprenex
buprenex
buprenex
buprenex
buprenophine
buprenophine
buprenophine
buprenorfina
buprenorfina
buprenorfine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
buprenorphine
(-)-buprenorphine
(-)-buprenorphine
(−)-buprenorphine
(−)-buprenorphine
buprenorphine hcl
buprenorphine hcl
buprenorphine hcl
buprenorphine hydrochloride
buprenorphine hydrochloride
buprenorphine hydrochloride
buprenorphine hydrochloride
buprenorphine hydrochloride, naloxone hydrochloride dihydrate
buprenorphine mixture with naloxone
buprenorphine / naloxone
buprenorphine/naloxone
buprenorphinum
buprenorphinum
butec
cam2038
cam2038
cl-112302
cl-112302
en3409
espranor
gabup
hapoctasin
indivior
natzon
nih-8805
nih-8805
nopan
norspan
norspan
norspan
panitaz
prefibin
prenotrix
probuphine
probuphine
reletrans
rx-6029m hcl
rx-6029m hcl
sevodyne
subutex
subutex
subutex
temgesic
temgesic
tephine
transtec
u- 952
u- 952

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT07176351	Phase 4	Dec 31, 2025	Yale University
NCT07097493	Phase 4	Dec 1, 2025	Atrium Medical Center, Wake Forest University
NCT06854029	Phase 4	Nov 30, 2025	Brown University, Duke University, Friends Research Institute, Inc., National Institute on Drug Abuse (NIDA), University of Arkansas
NCT06880718	Phase 4	Jun 30, 2025	Brown University, National Institute on Drug Abuse (NIDA)
NCT06949826	Phase 4	Apr 21, 2025	Washington University in St. Louis
NCT06772324	N/A	Jan 31, 2025	Peking University
NCT06726200	Phase 4	Jan 15, 2025	Columbia University, National Institute on Drug Abuse (NIDA)
NCT06742554	Phase 4	Dec 1, 2024	medina medical center
NCT06494904	Phase 3	Nov 30, 2024	Alameda Health System, National Drug Abuse Treatment Clinical Trials Network, National Institute on Drug Abuse (NIDA), The EMMES Corporation, Yale University
NCT06441604	Phase 2	Nov 1, 2024	Harvard University, University of Utah
NCT06379984	Phase 2	Nov 1, 2024	National Institute on Drug Abuse (NIDA), University of Pennsylvania
NCT06316830	N/A	Oct 1, 2024	Brown University, Rhode Island Hospital
NCT06576843	Phase 2	Sep 17, 2024	Indivior Inc.
NCT06442566	Phase 1/Phase 2 (Phase 2)	Aug 12, 2024	Medical University of South Carolina, National Institute on Drug Abuse (NIDA)
NCT06323824	Phase 4	Jun 4, 2024	Alameda Health System, Hennepin Healthcare, Kaiser Permanente, National Institute on Drug Abuse (NIDA), National Institutes of Health (NIH), The EMMES Corporation, University of California, San Francisco, Yale University
NCT06306443	Phase 3	Jun 1, 2024	Friends Research Institute, Inc.
NCT06367387	Phase 4	May 13, 2024	National Institute on Drug Abuse (NIDA), University of Pittsburgh
NCT06406400	Phase 2	May 13, 2024	AstraZeneca, Parexel
NCT06086275	Phase 1	Mar 31, 2024	Harvard University, University of Utah
NCT06051890	Phase 4	Jan 5, 2024	National Institute on Drug Abuse (NIDA), New York University

Showing 20 of 457 trials

Page 1 / 23

Organizations

Research & Development (265)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
National Institute on Drug Abuse (NIDA)	Government	134	47	5	1988
Indivior Inc.	For profit	34	28	5	2005
Purdue Pharmaceuticals	For profit	27	27	3	1996
University of Vermont	Academic/Hospital	25	10	2	1991
Yale University	Academic/Hospital	25	17	5	1988
Alkermes	For profit	23	20	3	2010
Johns Hopkins University	Academic/Hospital	22	13	5	1996
Mundipharma	For profit	20	18	5	2006
Columbia University	Academic/Hospital	19	18	5	1992
Friends Research Institute, Inc.	Academic/Hospital	19	7	3	1990
Department of Veteran Affairs	Government	15	5	3	1988
University of California, Los Angeles	Academic/Hospital	15	14	4	1990
University of Pennsylvania	Academic/Hospital	14	8	4	1992
BioDelivery Sciences International	For profit	13	12	4	2009
The EMMES Corporation	For profit	12	0	4	2011
Braeburn Pharmaceuticals	For profit	11	11	3	2006
Harvard University	Academic/Hospital	10	7	4	2007
New York University	Academic/Hospital	9	7	2	2014
University of Pittsburgh	Academic/Hospital	9	7	4	2010
Brown University	Academic/Hospital	8	5	4	2005

265 organizations

Page 1 / 14

Marketing (53)

Organization	Org type	Relationship	Date
Actavis	For profit	MKTG	Feb 22, 2013
Actavis	For profit	SYN	Oct 24, 2017
Alkem Labs Ltd	For profit	MKTG	Jun 15, 2021
Allergan PLC (2015)	For profit	MKTG	Oct 24, 2017
Alvogen	For profit	MKTG	Jan 24, 2019
Alvogen	For profit	MKTG	Aug 3, 2021
Amneal Pharmaceuticals	For profit	SYN	Apr 14, 2020
Amneal Pharmaceuticals	For profit	MKTG	Feb 22, 2013
Amneal Pharmaceuticals	For profit	SYN	Apr 14, 2020
Apotex	For profit	MKTG	Sep 23, 2021
Aveva Drug Delivery Systems	For profit	MKTG	Sep 23, 2021
Barr Laboratories	For profit	MKTG	May 7, 2010
BioDelivery Sciences International	For profit	NDA2	Jun 6, 2014
Braeburn Pharmaceuticals	For profit	NDA2	Dec 21, 2018
Braeburn Pharmaceuticals	For profit	MKTG	May 23, 2023
Bristol-Myers Squibb	For profit	MKTG	Jul 28, 2015
CASI Pharmaceuticals, Inc.	For profit	MKTG	Jun 10, 2015
Daiichi Sankyo	For profit	MKTG	Mar 27, 2007
Dr. Reddy's Laboratories	For profit	MKTG	Jun 14, 2018
Ethypharm	For profit	MKTG	Sep 24, 2010
Ethypharm	For profit	SYN	Oct 16, 2015
Hikma	For profit	MKTG	Oct 8, 2009
Hikma	For profit	MKTG	Mar 2, 2005
Hospira	For profit	MKTG	Jun 3, 1996
Indivior Inc.	For profit	NDA2	Dec 29, 1981
Indivior Inc.	For profit	SYN	Dec 29, 1981
Indivior Inc.	For profit	NDA	Dec 29, 1981
Lannett Company, Inc.	For profit	MKTG	Sep 19, 2016
Lutipold	For profit	MKTG	Mar 27, 2007
Mallinckrodt (2013)	For profit	MKTG	Dec 13, 2017
Mayne Pharma	For profit	MKTG	Jul 17, 2020
Mylan	For profit	SYN	Mar 6, 2015
Mylan	For profit	SYN	Mar 6, 2015
Mylan	For profit	MKTG	Jun 14, 2018
Mylan	For profit	MKTG	May 3, 2021
Norwich Eaton Company	For profit	NDA2	Dec 29, 1981
Orexo AB	For profit	MKTG	Jul 3, 2013
Orexo AB	For profit	NDA2	Jul 3, 2013
Par Pharmaceuticals	For profit	MKTG	Jul 28, 2015
Purdue Pharmaceuticals	For profit	NDA2	Jun 30, 2010
Rhodes Pharmaceuticals, L.P.	For profit	MKTG	Mar 27, 2017
Rubicon Research	For profit	MKTG	Jun 10, 2015
Sankyo	For profit	MKTG	Mar 27, 2007
Specgx Llc	For profit	MKTG	Dec 13, 2017
Sun Pharmaceuticals	For profit	SYN	Jan 19, 2022
Sun Pharmaceuticals	For profit	SYN	Jan 29, 2016
Sun Pharmaceuticals	For profit	MKTG	Jan 29, 2016
Teva	For profit	SYN	Sep 8, 2014
Teva	For profit	MKTG	Nov 20, 2018
Teva	For profit	NDA2	Sep 7, 2018
Titan Pharmaceuticals	For profit	NDA2	May 26, 2016
Wes Pharma Inc	For profit	MKTG	Jul 17, 2020
West-Ward Pharmaceutical	For profit	MKTG	Mar 2, 2005