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

General Information of Drug (ID: DM7B2JC)

• Drug Name: PF-05190457 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Type-2 diabetes	5A11	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 58438464
  CAS Number: CAS 1334782-79-4
  TTD Drug ID: DM7B2JC

Molecule-Related Drug Atlas

Drug(s) Targeting Growth hormone secretagogue receptor 1 (GHSR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GHRP-2	DMKGH0R	Growth hormone deficiency	5A61.3	Approved	[3]
Ibutamoren	DMFJ8LT	Fibromyalgia	MG30.01	Approved	[4]
Macimorelin	DMQYJIR	Growth hormone deficiency	5A61.3	Approved	[5]
Anamorelin	DM6HXTS	Carbohydrate metabolism disorder	5C51.Z	Phase 3	[6]
TZP-101	DMOE582	Gastrointestinal disease	DE2Z	Phase 2b	[7]
GTP-200	DM03NQS	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
RQ-00000005	DMBHN4K	Frailty	MG2A	Phase 2	[9]
Tabimorelin	DMNL9HO	Growth hormone deficiency	5A61.3	Phase 2	[10]
Ibutamoren mesylate	DMN2CM0	Growth hormone deficiency	5A61.3	Phase 2	[11]
Ipamorelin	DM9PJZT	Postoperative ileus	DA91-DB30	Phase 1/2	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Growth hormone secretagogue receptor 1 (GHSR)	TTWDC17	GHSR_HUMAN	Modulator	[2]

References

• [1] ClinicalTrials.gov (NCT01522807) A Study Of Three PF-05190457 Formulations In Healthy Volunteers. U.S. National Institutes of Health.
• [2] A gift for research. SciBX 7(6); doi:10.1038/scibx.2014.160. Feb. 13 2014
• [3] GH-releasing peptide-2 increases fat mass in mice lacking NPY: indication for a crucial mediating role of hypothalamic agouti-related protein. Endocrinology. 2002 Feb;143(2):558-68.
• [4] Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.
• [5] National Cancer Institute Drug Dictionary (drug id 735530).
• [6] Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers. Growth Horm IGF Res. 2009 Jun;19(3):267-73.
• [7] Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study. Clin Drug Investig. 2009;29(6):409-18.
• [8] Orphan GPCR research. Br J Pharmacol. 2008 March; 153(Suppl 1): S339-S346.
• [9] Hypotensive effects of ghrelin receptor agonists mediated through a novel receptor. Br J Pharmacol. 2014 Mar;171(5):1275-86.
• [10] Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol. 1999 Aug;141(2):180-9.
• [11] Effects of oral administration of ibutamoren mesylate, a nonpeptide growth hormone secretagogue, on the growth hormone-insulin-like growth factor I axis in growth hormone-deficient children. Clin Pharmacol Ther. 2001 Jul;70(1):91-8.
• [12] Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus.J Pharmacol Exp Ther.2009 Jun;329(3):1110-6.