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

General Information of Drug (ID: DMZTGN2)

• Drug Name: Methylnaltrexone bromide Drug Info
• Synonyms: Relistor; Methylnaltrexone (Bromide); Naltrexone methobromide; 73232-52-7; N-Methylnaltrexone Bromide; MRZ-2663BR; N-Cyclopropylmethyl-noroxymorphone Methobromide; Methylnaltrexone; MNTX; C21H26NO4Br; MOA-728; Relistor (TN); MRZ 2663BR; Naltrexone Methyl Bromide; N-Methyl Naltrexone Bromide; MNTX-302; SCHEMBL2798188; CHEMBL1201770; IFGIYSGOEZJNBE-KNLJMPJLSA-N; ONO-3849; Methylnaltrexone bromide (JAN/USAN); 3844AH; AKOS015896214; CS-0762; AN-37324; HY-75766; Methylnaltrexone bromide, > W-5330; CHIR-01020

Indication

Disease Entry	ICD 11	Status	REF
Opioid-induced constipation	DB32.1	Approved	[1]
Obesity	5B81	Preclinical	[2]

• Cross-matching ID:
  PubChem CID: 5361917
  CAS Number: CAS 73232-52-7
  TTD Drug ID: DMZTGN2
  ACDINA Drug ID: D01244

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	[3]
Morphine	DMRMS0L	Advanced cancer	2A00-2F9Z	Approved	[4]
Hydromorphone	DMHP21E	Back pain	ME84.Z	Approved	[5]
Tapentadol hydrochloride	DMXLSH3	Acute pain	MG31	Approved	[1]
Fentanyl	DM8WAHT	Analgesia	MB40.8	Approved	[6]
Alfentanil	DMVO0UB	Anaesthesia	9A78.6	Approved	[7]
Naloxegol	DML0B41	Opioid-induced constipation	DB32.1	Approved	[8]
Eluxadoline	DMYZ0P1	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[9]
Nalfurafine hcl	DMA9DHW	Uremic pruritus	EC90.10	Approved	[10]
Oxycodone	DMXLKHV	Osteoarthritis	FA00-FA05	Approved	[11]

Drug(s) Targeting Melanocortin receptor 4 (MC4R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bremelanotide	DM20LIM	Hypoactive sexual desire dysfunction	HA00	Approved	[12]
Setmelanotide	DMPVRN9	Obesity	5B81	Approved	[13]
Amylin	DMWDEN0	N. A.	N. A.	Phase 4	[14]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[2]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[15]
PF-446687	DML38VU	Female sexual arousal dysfunction	HA01.1	Phase 2	[16]
AP-1030	DMBGA35	Metabolic disorder	5C50-5D2Z	Phase 1/2	[17]
PF-07258669	DM3CJ5N	Malnutrition	5B50-5B71	Phase 1	[18]
PT-14	DMYM9JL	Erectile dysfunction	HA01.1	Discontinued in Phase 2	[19]
Melanotetan II	DMYK8MV	Obesity	5B81	Preclinical	[2]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Melanocortin receptor 4 (MC4R)	TTD0CIQ	MC4R_HUMAN	Agonist	[2]
Opioid receptor mu (MOP)	TTKWM86	OPRM_HUMAN	Modulator	[1]

References

• [1] 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
• [2] Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
• [3] Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
• [4] 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.
• [5] Clinical pipeline report, company report or official report of signaturerx.
• [6] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [7] 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.
• [8] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [9] Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
• [10] 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.
• [11] 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).
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [14] Novel anti-obesity drugs. Expert Opin Investig Drugs. 2000 Jun;9(6):1317-26.
• [15] Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
• [16] Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.
• [17] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [18] Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss. J Med Chem. 2023 Mar 9;66(5):3195-3211.
• [19] The protective effects of the melanocortin receptor (MCR) agonist, melanotan-II (MTII), against binge-like ethanol drinking are facilitated by deletion of the MC3 receptor in mice. Neuropeptides. 2014 Feb;48(1):47-51.