NALMEFENE HYDROCHLORIDE

US Previously Marketed

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H25NO3.ClH
Molecular Weight	375.889
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.[H][C@@]12OC3=C4C(C[C@H]5N(CC6CC6)CC[C@@]14[C@@]5(O)CCC2=C)=CC=C3O

InChI

InChIKey=GYWMRGWFQPSQLK-OPHZJPRHSA-N

InChI=1S/C21H25NO3.ClH/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13;/h4-5,13,16,19,23-24H,1-3,6-11H2;1H/t16-,19+,20+,21-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C21H25NO3
Molecular Weight	339.4281
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26810044 | https://www.ncbi.nlm.nih.gov/pubmed/25187751 | https://www.ncbi.nlm.nih.gov/pubmed/25302021 | https://www.medicines.org.uk/emc/medicine/27609

Nalmefene is the first medication approved for alcoholism with the primary goal of reducing alcohol intake in an as needed approach. Nalmefene received a marketing authorization valid throughout the European Union on February 25, 2013 and is under development in Asia. Nalmefene is an opioid system modulator with a distinct μ, δ, and κ receptor profile. In vitro studies have demonstrated that Nalmefene is a selective opioid receptor ligand with antagonist activity at the μ and δ receptors and partial agonist activity at the κ receptor. In vivo studies have demonstrated that nalmefene reduces alcohol consumption, possibly by modulating cortico-mesolimbic functions. In the US, immediate-release injectable nalmefene was approved in 1995 as an antidote for opioid overdose. It was sold under the trade name Revex. The product was discontinued by its manufacturer around 2008. Currently Nalmefene is sold under the trade name Selincro. Selincro is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking-risk level, without physical withdrawal symptoms and who do not require immediate detoxification.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Opioid receptors; mu/kappa/delta 33 Target ID: CHEMBL2095181 Sources: http://ec.europa.eu/health/documents/community-register/2013/20130225125325/anx_125325_en.pdf \| https://www.medicines.org.uk/emc/medicine/27609#PHARMACOLOGICAL_PROPS	Antagonist 2760
Mu opioid receptor 221 Target ID: CHEMBL233 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19027293 \| http://ec.europa.eu/health/documents/community-register/2013/20130225125325/anx_125325_en.pdf	Antagonist 2760	0.44 nM [Ki]
Delta opioid receptor 78 Target ID: CHEMBL236 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19027293 \| http://ec.europa.eu/health/documents/community-register/2013/20130225125325/anx_125325_en.pdf	Antagonist 2760	9.3 nM [Ki]
Kappa opioid receptor 108 Target ID: CHEMBL237 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19027293 \| http://ec.europa.eu/health/documents/community-register/2013/20130225125325/anx_125325_en.pdf	Partial Agonist 288	0.12 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alcoholism 19 Sources: http://ec.europa.eu/health/documents/community-register/2013/20130225125325/anx_125325_en.pdf	Primary		Approved 8360	Selincro Approved Use Selincro is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking-risk level, without physical withdrawal symptoms and who do not require immediate detoxification. Launch Date 1.36175039E12

C_max

Value	Dose	Analyte	Population
155 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
177 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
57.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
109 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1320 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
16.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8877019/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
16.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1876 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
191 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
274 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
29.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8877019/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
314 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
385 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	24 mg single, intravenous dose: 24 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
647 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
8.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8877019/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
11.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8877019/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
9.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
8.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3943269/	24 mg single, intravenous dose: 24 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3680580/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NALMEFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
18 mg 1 times / day steady, oral Recommended Dose: 18 mg, 1 times / day Route: oral Route: steady Dose: 18 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30829564/	unhealthy, 39 years n = 1 Health Status: unhealthy Condition: alcohol dependence and Schizoaffective Disorder Age Group: 39 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/30829564/	Disc. AE: Psychiatric decompensation... AEs leading to discontinuation/dose reduction: Psychiatric decompensation (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/30829564/
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/	healthy, adult n = 4 Health Status: healthy Age Group: adult Sex: M Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/	Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/	healthy, adult n = 4 Health Status: healthy Age Group: adult Sex: M Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/	Sources: https://pubmed.ncbi.nlm.nih.gov/3680580/
0.75 ug/kg single, intravenous Highest studied dose Dose: 0.75 ug/kg Route: intravenous Route: single Dose: 0.75 ug/kg Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	unhealthy, adult n = 3 Health Status: unhealthy Condition: postoperative pain Age Group: adult Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	DLT: Anesthesia reversal... Dose limiting toxicities: Anesthesia reversal (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/
0.5 ug/kg single, intravenous MTD Dose: 0.5 ug/kg Route: intravenous Route: single Dose: 0.5 ug/kg Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	unhealthy, adult n = 18 Health Status: unhealthy Condition: postoperative pain Age Group: adult Sex: M+F Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	DLT: Anesthesia reversal... Dose limiting toxicities: Anesthesia reversal (3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/
20 mg 2 times / day steady, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: steady Dose: 20 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	unhealthy, adult n = 7 Health Status: unhealthy Condition: alcohol dependence Age Group: adult Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	Disc. AE: Dizziness... AEs leading to discontinuation/dose reduction: Dizziness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/
5 mg 2 times / day steady, oral Studied dose Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	unhealthy, adult n = 7 Health Status: unhealthy Condition: alcohol dependence Age Group: adult Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	Disc. AE: Dizziness, Rash... AEs leading to discontinuation/dose reduction: Dizziness (1 patient) Rash (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/

AEs

AE	Significance	Dose	Population
Psychiatric decompensation	1 patient Disc. AE	18 mg 1 times / day steady, oral Recommended Dose: 18 mg, 1 times / day Route: oral Route: steady Dose: 18 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30829564/	unhealthy, 39 years n = 1 Health Status: unhealthy Condition: alcohol dependence and Schizoaffective Disorder Age Group: 39 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/30829564/
Anesthesia reversal	2 patients DLT	0.75 ug/kg single, intravenous Highest studied dose Dose: 0.75 ug/kg Route: intravenous Route: single Dose: 0.75 ug/kg Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	unhealthy, adult n = 3 Health Status: unhealthy Condition: postoperative pain Age Group: adult Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/
Anesthesia reversal	3 patients DLT	0.5 ug/kg single, intravenous MTD Dose: 0.5 ug/kg Route: intravenous Route: single Dose: 0.5 ug/kg Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/	unhealthy, adult n = 18 Health Status: unhealthy Condition: postoperative pain Age Group: adult Sex: M+F Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/10754620/
Dizziness	1 patient Disc. AE	20 mg 2 times / day steady, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: steady Dose: 20 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	unhealthy, adult n = 7 Health Status: unhealthy Condition: alcohol dependence Age Group: adult Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/
Dizziness	1 patient Disc. AE	5 mg 2 times / day steady, oral Studied dose Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	unhealthy, adult n = 7 Health Status: unhealthy Condition: alcohol dependence Age Group: adult Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/
Rash	1 patient Disc. AE	5 mg 2 times / day steady, oral Studied dose Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/	unhealthy, adult n = 7 Health Status: unhealthy Condition: alcohol dependence Age Group: adult Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7847600/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inducer 383 inhibitor 1752		inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1437 BCRP 691 MRP2 367 OATP1B1 781 OATP1B3 700 OCT1 506 CYP1A2 1509 CYP2A6 704 CYP2B6 799 CYP2C8 901 CYP2C19 1463 CYP3A4/5 273	UGT2B7 389 UGT1A3 422 UGT1A8 283 sulfotransferases 36 CYP3A4/5 85 P-gp 1527 BCRP 555 MRP2 201 OATP1B1 403 OATP1B3 347 OCT1 322	CYP1A2 689 CYP2A6 79 CYP2B6 538 CYP2C8 168 CYP2C19 290 CYP3A4/5 120

Drug as perpetrator

Target	Modality	Activity
BCRP 765	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
CYP1A2 1673	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2A6 736	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2A6 736	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2B6 985	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2B6 985	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C19 1537	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C8 955	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C8 955	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C9 1803	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP3A4/5 330	inducer 1542 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
CYP3A4/5 330	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=23 Page: 23.0	no
MRP2 459	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OATP1B1 796	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OATP1B3 709	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OCT1 523	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
P-gp 1626	inhibitor 3240 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no

Drug as victim

Target	Modality	Activity
UGT1A3 422	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/product-information/selincro-epar-product-information_en.pdf#page=11 Page: 11.0	minor
UGT1A8 283	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/product-information/selincro-epar-product-information_en.pdf#page=11 Page: 11.0	minor
BCRP 555	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
MRP2 201	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OATP1B1 403	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OATP1B3 347	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
OCT1 322	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
P-gp 1527	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=14 Page: 14.0	no
CYP3A4/5 85	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/product-information/selincro-epar-product-information_en.pdf#page=11 Page: 11.0	yes
UGT2B7 389	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/product-information/selincro-epar-product-information_en.pdf#page=10 Page: 10.0	yes
sulfotransferases 36	substrate 3326 Sources: https://www.ema.europa.eu/en/documents/product-information/selincro-epar-product-information_en.pdf#page=11 Page: 11.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.ema.europa.eu/en/documents/assessment-report/selincro-epar-public-assessment-report_en.pdf#page=12 Page: 12.0

Sourcing

Vendor/Aggregator	ID	URL
AK Scientific, Inc. (AKSCI)	67672	http://www.aksci.com/item_detail.php?cat=67672
Achemtek	0104-005955	http://www.achemtek.com/55096-26-9
Alfa Chemistry	55096-26-9	https://www.alfa-chemistry.com/cas_55096-26-9.htm
Ambinter	Amb17618203	http://www.ambinter.com/reference/17618203
Ambinter	Amb22801010	http://www.ambinter.com/reference/22801010
ApexBio Technology	B5505	http://www.apexbt.com/nalmefene-d3.html
Aurora Fine Chemicals LLC	A17.877.204	http://online.aurorafinechemicals.com/info?ID=A17.877.204
BioChemPartner	BCP16723	http://www.biochempartner.com/55096-26-9-BCP16723
BioCrick	BCC6093	http://www.biocrick.com/Nalmefene-d3-BCC6093.html
ChemMol	49425127	http://www.chemmol.com/chemmol/49425127.html
ChemMol	99105242	http://www.chemmol.com/chemmol/99105242.html
Chemspace	CSSB00020660084	https://chem-space.com/CSSB00020660084
DC Chemicals	DC37635	http://www.dcchemicals.com//product_show-Nalmefene.html
Glentham Life Sciences	GP5746	http://www.glentham.com/products/product/GP5746/
Lab Network	LN01291034	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01291034
OChem	5964	http://www.ocheminc.com/index.php?act=psearch&pid=096N269
Sigma-Aldrich	N5770_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/n5770?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S536625	http://www.smolecule.com/products/s536625
THE BioTek	bt-276130	https://www.thebiotek.com/product/inhibitors/bt-276130

PubMed

Title	Date	PubMed
Nalmefene: intravenous safety and kinetics of a new opioid antagonist.	1986 Jan	3943269
The role of endogenous opioids in congestive heart failure: effects of nalmefene on systemic and regional hemodynamics in dogs.	1987 Feb	3026683
A double-blind, placebo-controlled pilot study to evaluate the efficacy and safety of oral nalmefene HCl for alcohol dependence.	1994 Oct	7847600
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.	1998 Mar	9686407
Dynorphin A1-13 causes elevation of serum levels of prolactin through an opioid receptor mechanism in humans: gender differences and implications for modulation of dopaminergic tone in the treatment of addictions.	1999 Jan	9862779
Use of acamprosate and opioid antagonists in the treatment of alcohol dependence: a European perspective.	2003	14972781
[Drug therapy of alcohol dependence--a critical review].	2003	14870516
Pharmacotherapy of alcohol dependence: a review of the clinical data.	2004	15182219
A multi-site dose ranging study of nalmefene in the treatment of alcohol dependence.	2004 Aug	15232334
Chronic administration of nalmefene leads to increased food intake and body weight gain in mice.	2004 Jul 8	15219821
Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice.	2004 Mar 5	14759503
Pharmacotherapy for erectile dysfunction.	2004 Sep	16422967
Effects of naltrexone and nalmefene on subjective response to alcohol among non-treatment-seeking alcoholics and social drinkers.	2004 Sep	15365307
Implantable technology for long-term delivery of nalmefene for treatment of alcoholism.	2004 Sep 28	15363499
Stimulation of the hypothalamic-pituitary-adrenal axis with the opioid antagonist nalmefene.	2005	16379031
Determination of nalmefene by high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry.	2005 Apr	15842759
Nalmefene induced elevation in serum prolactin in normal human volunteers: partial kappa opioid agonist activity?	2005 Dec	15988468
Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing.	2005 Dec	15956985
Opioid antagonists for alcohol dependence.	2005 Jan 25	15674887
Unexpected placebo response in premenstrual dysphoric disorder: implication of endogenous opioids.	2005 Oct	16001107
Comorbidity issues in the pharmacological treatment of Pathological Gambling: a critical review.	2005 Oct 10	16216125
Phobic memory and somatic vulnerabilities in anorexia nervosa: a necessary unity?	2005 Sep 6	16144551
Acamprosate: a new tool in the battle against alcohol dependence.	2006 Dec	19412493
The permeation of nalmefene hydrochloride across different regions of ovine nasal mucosa.	2006 Dec	17139110
Epidemiologic and clinical updates on impulse control disorders: a critical review.	2006 Dec	16960655
Multicenter investigation of the opioid antagonist nalmefene in the treatment of pathological gambling.	2006 Feb	16449486
Pathological gambling: focusing on the addiction, not the activity.	2006 Feb	16449466
Optimization of the preparation of nalmefene-loaded sustained-release microspheres using central composite design.	2006 Jul	16819215
Pharmacologic treatments for opioid dependence: detoxification and maintenance options.	2007	18286804
Pharmacoprophylaxis of alcohol dependence: Review and update Part I: Pharmacology.	2007 Jan	20640061
Effects of salvinorin A, a kappa-opioid hallucinogen, on a neuroendocrine biomarker assay in nonhuman primates with high kappa-receptor homology to humans.	2007 Jan	17060493
Plasma met-enkephalin, beta-endorphin and leu-enkephalin levels in human hepatic encephalopathy.	2007 Mar-Apr	17684846
Evidence of accelerated ageing in clinical drug addiction from immune, hepatic and metabolic biomarkers.	2007 Sep 24	17892544
Effects of opioid receptor gene variation on targeted nalmefene treatment in heavy drinkers.	2008 Jul	18537939
Cholestatic hepatitis as a possible new side-effect of oxycodone: a case report.	2008 May 1	18452597
Opioid antagonists for pharmacological treatment of alcohol dependence - a critical review.	2008 Nov	19630726
Predicting response to opiate antagonists and placebo in the treatment of pathological gambling.	2008 Nov	18581096
Agenda for specialty section in addiction medicine.	2008 Oct	19823604
Primary biliary cirrhosis.	2009 Sep	19603170
The Effects of Naltrexone Among Alcohol Non-Abstainers: Results from the COMBINE Study.	2010	21423437
Pediatric sedation: a global challenge.	2010	20981309
Human exposures to immobilising agents: results of an online survey.	2010 Aug 28	20802186
Emerging drugs to treat alcoholism.	2010 Dec	20560783
Opioid antagonists for alcohol dependence.	2010 Dec 8	21154349
Opioid antagonists under heavy sedation or anaesthesia for opioid withdrawal.	2010 Jan 20	20091529
[Clinical observation of the effect of nalmefene in treatment of septic shock].	2010 Jun	20594468
[Serum NT-proBNP levels in neonates with severe asphyxia and the effects of nalmefene on the NT-proBNP levels].	2010 Nov	21083993
Nalmefene in the treatment of pathological gambling: multicentre, double-blind, placebo-controlled study.	2010 Oct	20884959
Brain imaging studies in pathological gambling.	2010 Oct	20676945
Long-term efficacy, tolerability and safety of nalmefene as-needed in patients with alcohol dependence: A 1-year, randomised controlled study.	2014 Aug	24671340

Patents

Sample Use Guides

In Vivo Use Guide

How much to take - The recommended dose is one tablet on days when you think there is a risk you will drink alcohol - The maximum dose is one tablet per day. How and when to take - You should take the tablet 1-2 hours before you start drinking alcohol. - Swallow the tablet whole, do not crush or divide the tablet. - You can take Selincro (Nalmefene) with or without food. Each film-coated tablet contains 18.06 mg nalmefene (as hydrochloride dihydrate).

Route of Administration: Oral

In Vitro Use Guide

Nalmefene antagonized the bindings of [3H]-dihydromorphine, [3H]-ethylketocyclazocine and [3H]-D-ala-D-leu enkephalin with IC50's in the low nanomolar range in rat brain membranes.. At the central mu receptor, nalmefene bound with an IC50 of 1.0 nM

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:16:31 UTC 2023` Edited by `admin` on `Wed Jul 05 23:16:31 UTC 2023`
Record UNII	K7K69QC05X
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NALMEFENE HYDROCHLORIDE

Common Name

English

Nalmefene hydrochloride [WHO-DD]

Common Name

English

JF-1 HYDROCHLORIDE

Code

English

NALMEFENE HYDROCHLORIDE [VANDF]

Common Name

English

NALMEFENE HCL

Common Name

English

OPVEE

Brand Name

English

NALMEFENE HYDROCHLORIDE [MART.]

Common Name

English

17-CYCLOPROPYLMETHYL-4,5A-EPOXY-6-METHYLENEMORPHINAN-3,14-DIOL HYDROCHLORIDE

Common Name

English

NALMEFENE HYDROCHLORIDE [MI]

Common Name

English

NALMEFENE HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

REVEX

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C681