U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C25H32N2O4.2H2O
Molecular Weight 460.5631
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ALVIMOPAN

SMILES

O.O.C[C@H]1CN(C[C@H](CC2=CC=CC=C2)C(=O)NCC(O)=O)CC[C@@]1(C)C3=CC=CC(O)=C3

InChI

InChIKey=USPVLEIQIUNQGE-DBFLIVQGSA-N
InChI=1S/C25H32N2O4.2H2O/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19;;/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30);2*1H2/t18-,20-,25+;;/m0../s1

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8057274 | http://adisinsight.springer.com/drugs/800003539

Alvimopan (LY246736, ADL 8-2698, trade name Entereg) is a potent, peripherally selective mu-opioid receptor antagonist. Alvimopan was developed by Adolor Corporation (now Cubist Pharmaceuticals) and GlaxoSmithKline for the treatment of postoperative ileus. Postoperative ileus is the impairment of gastrointestinal motility after intra-abdominal surgery or other non-abdominal surgeries. This may potentially delay gastrointestinal recovery and hospital discharge until its resolution. Morphine and other mu-opioid receptor agonists are universally used for the treatment of acute postsurgical pain; however, they are known to have an inhibitory effect on gastrointestinal motility and may prolong the duration of postoperative ileus. Following oral administration, alvimopan antagonizes the peripheral effects of opioids on gastrointestinal motility and secretion by competitively binding to gastrointestinal tract mu-opioid receptors.

CNS Activity

Originator

Eli Lilly
237
Curator's Comment: # Eli Lilly

Approval Year

2008
174
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 0.77 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
Approved
8429
ENTEREG

Approved Use

ENTEREG is a peripherally acting μ-opioid receptor antagonist indicated to accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis.

Launch Date

2008
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
10.98 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day multiple, oral
dose: 12 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALVIMOPAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
40.2 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day multiple, oral
dose: 12 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALVIMOPAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
13.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day multiple, oral
dose: 12 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALVIMOPAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day multiple, oral
dose: 12 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALVIMOPAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
120 mg single, oral
Highest studied dose
Dose: 120 mg
Route: oral
Route: single
Dose: 120 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
48 mg 1 times / day multiple, oral
Highest studied dose
Dose: 48 mg, 1 times / day
Route: oral
Route: multiple
Dose: 48 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021775lbl.pdf
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Other AEs: Ascites, Ileus...
Other AEs:
Ascites (serious, 1 patient)
Ileus (serious, 1 patient)
Electrolyte imbalance (serious, 1 patient)
Failure to thrive (serious, 1 patient)
Syncope (serious, 1 patient)
Wound infection (serious, 2 patients)
Wound complication (serious, 1 patient)
Mania (serious, 1 patient)
Hypertension (below serious, 3 patients)
Constipation (below serious, 18 patients)
Diarrhea (below serious, 6 patients)
Dyspepsia (below serious, 1 patient)
Nausea (below serious, 20 patients)
Vomiting (below serious, 9 patients)
Anorexia (below serious, 4 patients)
Esophagitis (below serious, 1 patient)
Gastroparesis (below serious, 1 patient)
Weight loss (below serious, 3 patients)
Leukocytosis (below serious, 4 patients)
International normalized ratio increased (below serious, 1 patient)
Electrolyte imbalance (below serious, 8 patients)
Hypomagnesemia (below serious, 2 patients)
Elevated liver enzymes (below serious, 2 patients)
Delirium (below serious, 3 patients)
Insomnia (below serious, 1 patient)
Sensory neuropathy (below serious, 3 patients)
Cystostomy (below serious, 1 patient)
Pelvic abscess (below serious, 1 patient)
Urinary tract obstruction (below serious, 1 patient)
Allergic reaction to chemotherapy (below serious, 1 patient)
Pneumonitis (below serious, 2 patients)
Pneumothorax (below serious, 2 patients)
Wound infection (below serious, 7 patients)
Skin infection (below serious, 2 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
AEs

AEs

AESignificanceDosePopulation
Allergic reaction to chemotherapy below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Cystostomy below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Dyspepsia below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Esophagitis below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Gastroparesis below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Insomnia below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
International normalized ratio increased below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Pelvic abscess below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Urinary tract obstruction below serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Constipation below serious, 18 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Elevated liver enzymes below serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Hypomagnesemia below serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Pneumonitis below serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Pneumothorax below serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Skin infection below serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Nausea below serious, 20 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Delirium below serious, 3 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Hypertension below serious, 3 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Sensory neuropathy below serious, 3 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Weight loss below serious, 3 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Anorexia below serious, 4 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Leukocytosis below serious, 4 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Diarrhea below serious, 6 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Wound infection below serious, 7 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Electrolyte imbalance below serious, 8 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Vomiting below serious, 9 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Ascites serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Electrolyte imbalance serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Failure to thrive serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Ileus serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Mania serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Syncope serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Wound complication serious, 1 patient
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Wound infection serious, 2 patients
12 mg 2 times / day steady, oral
Dose: 12 mg, 2 times / day
Route: oral
Route: steady
Dose: 12 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
unhealthy
n = 66
Health Status: unhealthy
Condition: ovarian cancer
Population Size: 66
Sources:
https://clinicaltrials.gov/ct2/show/NCT01704651
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882

P-gp
1461
CYP
270

P-gp
1537
CYP1A2
701

CYP2B6
547

CYP2C19
293

CYP3A4/5
124
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no [IC50 >50 uM]
CYP2A6
739
 no [IC50 >50 uM]
CYP2B6
1001
 no [IC50 >50 uM]
CYP2C19
1553
 no [IC50 >50 uM]
CYP2C8
965
 no [IC50 >50 uM]
CYP2C9
1819
 no [IC50 >50 uM]
CYP2D6
1891
 no [IC50 >50 uM]
CYP2E1
970
 no [IC50 >50 uM]
CYP3A4
1925
 no [IC50 >50 uM]
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C9
1819
 no
CYP3A4/5
335
 no
P-gp
1650
 no
no (co-administration study)
Comment: based on study using MDCKII cells, digoxin transport not affected
Page: 66, 67
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP
270
 no
P-gp
1537
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
PubMed

PubMed

TitleDatePubMed
Use of selective opiate receptor inhibitors to prevent postoperative ileus.
2002 Apr
Alvimopan (Adolor/GlaxoSmithKline).
2002 Oct
Opioid-induced bowel dysfunction: pathophysiology and potential new therapies.
2003
Postoperative ileus: etiologies and interventions.
2003 Mar
Alvimopan: an oral, peripherally acting, mu-opioid receptor antagonist for the treatment of opioid-induced bowel dysfunction--a 21-day treatment-randomized clinical trial.
2005 Mar
Alvimopan: ADL 8-2698, ADL 82698, Entrareg, LY 246736.
2006
Current choices--good or bad--for the proactive management of postoperative ileus: A surgeon's view.
2006 Apr
Use of novel prokinetic agents to facilitate return of gastrointestinal motility in adult critically ill patients.
2006 Aug
The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats.
2006 Aug 2
Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study.
2006 Jan
Novel opioid antagonists for opioid-induced bowel dysfunction and postoperative ileus.
2007
Patterns of gastrointestinal recovery after bowel resection and total abdominal hysterectomy: pooled results from the placebo arms of alvimopan phase III North American clinical trials.
2007 Jul
Cancer-related constipation.
2007 Jul
Pharmacologic management of postoperative ileus: the next chapter in GI surgery.
2007 Mar
Is alvimopan a safe and effective treatment for postoperative ileus?
2007 Sep
Clinical trial: alvimopan for the management of post-operative ileus after abdominal surgery: results of an international randomized, double-blind, multicentre, placebo-controlled clinical study.
2008 Aug 1
The involvement of the mu-opioid receptor in gastrointestinal pathophysiology: therapeutic opportunities for antagonism at this receptor.
2008 Jan
Opioid-induced bowel dysfunction.
2008 Jan
New drug to restore bowel function approved under new FDA rules.
2008 Jul 1
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
2008 Mar 15
Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus.
2008 Oct
Development of peripheral opioid antagonists' new insights into opioid effects.
2008 Oct
Efficacy and safety of mu-opioid antagonists in the treatment of opioid-induced bowel dysfunction: systematic review and meta-analysis of randomized controlled trials.
2008 Sep
[News from the cochrane library: mu opioid antagonists for opioid-induced bowel dysfunction].
2008 Sep
New drugs: methylnaltrexone bromide, alvimopan, and rilonacept.
2008 Sep-Oct
Novel opioid antagonists for opioid-induced bowel dysfunction and postoperative ileus.
2009 Apr 4
Alvimopan for postoperative ileus: only one piece of the puzzle.
2009 Jul 15
Alvimopan for postoperative ileus.
2009 Jul 15
Preventing paralytic ileus: can the anesthesiologist help.
2009 Jun
Peripherally acting mu-opioid receptor antagonists and postoperative ileus: mechanisms of action and clinical applicability.
2009 Jun
Opioid receptors in the gastrointestinal tract.
2009 Jun 5
Comment on alvimopan guidelines.
2009 Sep
Pharmacologic options to prevent postoperative ileus.
2009 Sep
The effects of a short course of antibiotics on alvimopan and metabolite pharmacokinetics.
2010 Mar
Gastrointestinal recovery after laparoscopic colectomy: results of a prospective, observational, multicenter study.
2010 Mar
Patents

Patents

JP4343948B2
9
WO2007047935A1
3
WO2011161646A2
3
WO2013080221A2
3

Sample Use Guides

In Vivo Use Guide
12 mg administered 30 minutes to 5 hours prior to surgery followed by 12 mg twice daily for up to 7 days for a maximum of 15 doses
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: In morphine-naive guinea pig ileum alvimopan increased, the amplitude of electrically evoked contractions and spontaneous mechanical activity.
Unknown
Name Type Language
ALVIMOPAN
DASH   HSDB   ORANGE BOOK   USAN   VANDF  
USAN  
Official Name English
ENTEREG
Brand Name English
ALVIMOPAN DIHYDRATE [MI]
Common Name English
ALVIMOPAN [VANDF]
Common Name English
LY-246736
Code English
ALVIMOPAN [ORANGE BOOK]
Common Name English
ADL-8-2698
Code English
ALVIMOPAN [HSDB]
Common Name English
[[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl]-3-phenylpropanoyl]amino]acetic acid dihydrate
Systematic Name English
LY-246736 DIHYDRATE
Code English
ALVIMOPAN [USAN]
Common Name English
ADL 8-2698
Code English
LY246736
Code English
ALVIMOPAN DIHYDRATE [MART.]
Common Name English
GLYCINE, N-(2-((4-(3-HYDROXYPHENYL)-3,4-DIMETHYL-1-PIPERIDINYL)METHYL)-1-OXO-3-PHENYLPROPYL)-, DIHYDRATE, (3R-(1(S*),3.ALPHA.,4.ALPHA.))-
Common Name English
ALVIMOPAN DIHYDRATE
MART.   MI  
Common Name English
Classification Tree Code System Code
WHO-VATC QA06AH02
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
NCI_THESAURUS C681
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
WHO-ATC A06AH02
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
NDF-RT N0000175691
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
Code System Code Type Description
MERCK INDEX
m1636
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY Merck Index
NCI_THESAURUS
C49096
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
USAN
MM-72
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
DRUG CENTRAL
143
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
DRUG BANK
DB06274
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
FDA UNII
677C126AET
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
MESH
C419502
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
ChEMBL
CHEMBL270190
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
SMS_ID
300000032193
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
PUBCHEM
5488547
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
WIKIPEDIA
ALVIMOPAN
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
EPA CompTox
DTXSID40168794
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
DAILYMED
677C126AET
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
IUPHAR
7471
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
CAS
170098-38-1
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY
RXCUI
480639
Created by admin on Fri Dec 15 16:02:41 GMT 2023 , Edited by admin on Fri Dec 15 16:02:41 GMT 2023
PRIMARY RxNorm
SUBSTANCE RECORD
Structure of ALVIMOPAN
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966