Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C26H39N3O4 |
Molecular Weight | 457.6056 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)C1=CC=CC(=C1)[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(CC4CCCCC4)C(=O)[C@@H](O)CO
InChI
InChIKey=ATLYLVPZNWDJBW-KIHHCIJBSA-N
InChI=1S/C26H39N3O4/c27-25(32)20-8-4-7-19(13-20)21-14-22-9-10-23(15-21)29(22)12-11-28(26(33)24(31)17-30)16-18-5-2-1-3-6-18/h4,7-8,13,18,21-24,30-31H,1-3,5-6,9-12,14-17H2,(H2,27,32)/t21-,22+,23-,24-/m0/s1
Axelopran (previously known as TD-1211), a peripherally selective, multivalent µ-opioid receptor antagonist that is under development by Theravance Biopharma. This drug participated in phase II clinical trials in subjects with opioid-induced constipation. The most common adverse events were abdominal pain, nausea, and diarrhea. There were no indications of opioid withdrawal effects or reductions in opioid analgesia in patients treated with axelopran.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Novel Oral Therapies for Opioid-induced Bowel Dysfunction in Patients with Chronic Noncancer Pain. | 2016 Mar |
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Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists. | 2017 Jul 1 |
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Clinical Overview and Considerations for the Management of Opioid-induced Constipation in Patients With Chronic Noncancer Pain. | 2019 Feb |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01401985
Capsules once daily
Route of Administration:
Oral
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Axelopran
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9789
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C171856
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300000034121
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85U7ROB149
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DB12013
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BC-61
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949904-48-7
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CHEMBL3137313
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DTXSID301032386
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)