Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMHR8KW)

• Drug Name: Alvimopan Drug Info
• Synonyms: Alvimopan anhydrous; LY 246736; LY246736; Adl 8-2698; Entereg (TN); Trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine; Glycine, N-[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl; 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid

Indication

Disease Entry	ICD 11	Status	REF
Gastrointestinal disease	DE2Z	Approved	[1]

• Therapeutic Class: Analgesics
• Cross-matching ID:
  PubChem CID: 5488548
  ChEBI ID: CHEBI:135686
  CAS Number: CAS 156053-89-3
  TTD Drug ID: DMHR8KW
  ACDINA Drug ID: D00026

Molecule-Related Drug Atlas

Drug(s) Targeting Opioid receptor mu (MOP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Buprenorphine	DMPRI8G	Opioid dependence	6C43.2Z	Approved	[4]
Morphine	DMRMS0L	Advanced cancer	2A00-2F9Z	Approved	[5]
Hydromorphone	DMHP21E	Back pain	ME84.Z	Approved	[6]
Tapentadol hydrochloride	DMXLSH3	Acute pain	MG31	Approved	[7]
Fentanyl	DM8WAHT	Analgesia	MB40.8	Approved	[8]
Alfentanil	DMVO0UB	Anaesthesia	9A78.6	Approved	[9]
Naloxegol	DML0B41	Opioid-induced constipation	DB32.1	Approved	[10]
Eluxadoline	DMYZ0P1	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[11]
Nalfurafine hcl	DMA9DHW	Uremic pruritus	EC90.10	Approved	[12]
Oxycodone	DMXLKHV	Osteoarthritis	FA00-FA05	Approved	[13]

Drug(s) Affected By Mu-type opioid receptor (OPRM1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fentanyl	DM8WAHT	Analgesia	MB40.8	Approved	[14]
Morphine	DMRMS0L	Advanced cancer	2A00-2F9Z	Approved	[15]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[16]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[17]
Butorphanol	DM5KYPJ	Pain	MG30-MG3Z	Approved	[18]
Oliceridine	DM6MDCF	Acute pain	MG31	Approved	[14]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[19]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[20]
Decitabine	DMQL8XJ	Acute myelogenous leukaemia	2A41	Approved	[21]
Tianeptine	DMYN8MA	Major depressive disorder	6A70.3	Approved	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor mu (MOP)	TTKWM86	OPRM_HUMAN	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Mu-type opioid receptor (OPRM1)	OT16AAT8	OPRM_HUMAN	Protein Interaction/Cellular Processes	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7471).
• [2] Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77.
• [3] The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexone. Naunyn Schmiedebergs Arch Pharmacol. 2007 May;375(3):205-20. doi: 10.1007/s00210-007-0146-x. Epub 2007 Mar 6.
• [4] Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
• [5] Antianalgesia: stereoselective action of dextro-morphine over levo-morphine on glia in the mouse spinal cord.J Pharmacol Exp Ther.2005 Sep;314(3):1101-8.
• [6] Clinical pipeline report, company report or official report of signaturerx.
• [7] 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
• [8] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [9] Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87.
• [10] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [11] Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
• [12] Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
• [13] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 319).
• [14] A G protein-biased ligand at the ?-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17.
• [15] Association of ABCB1/MDR1 and OPRM1 gene polymorphisms with morphine pain relief. Clin Pharmacol Ther. 2008 Apr;83(4):559-66.
• [16] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [17] The effect of mitragynine on cAMP formation and mRNA expression of mu-opioid receptors mediated by chronic morphine treatment in SK-N-SH neuroblastoma cell. J Ethnopharmacol. 2013 Jun 21;148(1):135-43. doi: 10.1016/j.jep.2013.03.078. Epub 2013 Apr 19.
• [18] In vitro functional characterization of a panel of non-fentanyl opioid new psychoactive substances. Arch Toxicol. 2020 Nov;94(11):3819-3830. doi: 10.1007/s00204-020-02855-7. Epub 2020 Jul 31.
• [19] Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells. Mol Pharmacol. 2006 Apr;69(4):1486-91. doi: 10.1124/mol.105.018325. Epub 2006 Jan 24.
• [20] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [21] Regulation of opioid and cannabinoid receptor genes in human neuroblastoma and T cells by the epigenetic modifiers trichostatin A and 5-aza-2'-deoxycytidine. Neuroimmunomodulation. 2012;19(3):180-6. doi: 10.1159/000331474. Epub 2012 Jan 18.