Gemopatrilat

Gemopatrilat
Clinical data
Other names	BMS-189921
ATC code	None;
Identifiers
	IUPAC name (6S)-Hexahydro-6-[(αS)-α-mercaptohydrocinnamido]-2,2-dimethyl-7-oxo-1H-azepine-1-acetic acid;
CAS Number	160135-92-2;
PubChem CID	9886079;
ChemSpider	8061752;
UNII	MU9089C77W;
KEGG	D04312;
ChEMBL	ChEMBL107747;
Chemical and physical data
Formula	C19H26N2O4S
Molar mass	378.49 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1(CCC[C@@H](C(=O)N1CC(=O)O)NC(=O)[C@H](CC2=CC=CC=C2)S)C;
	InChI InChI=1S/C19H26N2O4S/c1-19(2)10-6-9-14(18(25)21(19)12-16(22)23)20-17(24)15(26)11-13-7-4-3-5-8-13/h3-5,7-8,14-15,26H,6,9-12H2,1-2H3,(H,20,24)(H,22,23)/t14-,15-/m0/s1; Key:YRSVDSQRGBYVIY-GJZGRUSLSA-N;

Gemopatrilat (INN)[1] is an experimental drug that was never marketed.[2] It acts as a vasopeptidase inhibitor.[3][4] It inhibits both angiotensin-converting enzyme (ACE) and neutral endopeptidase (neprilysin).[5]

References

"International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 46" (PDF). World Health Organization. p. 200. Retrieved 2 March 2017.
"Gemopatrilat". AdisInsight. Highest Development Phases: Discontinued
Laverman, GD; Van Goor, H; Henning, RH; De Jong, PE; De Zeeuw, D; Navis, G (January 2003). "Renoprotective Effects of VPI Versus ACEI in Normotensive Nephrotic Rats on Different Sodium Intakes". Kidney International. 63 (1): 64–71. doi:10.1046/j.1523-1755.2003.00708.x. PMID 12472769. Retrieved 2 March 2017.
Wait, JC; Vaccharajani, N; Mitroka, J; Jemal, M; Khan, S; Bonacorsi, SJ; Rinehart, JK; Iyer, RA (June 2006). "Metabolism of [¹⁴C]Gemopatrilat After Oral Administration to Rats, Dogs, and Humans" (PDF). Drug Metabolism and Disposition. 34 (6): 961–70. doi:10.1124/dmd.105.007500. PMID 16540589. Retrieved 2 March 2017.
Hubner, RA; Kubota, E; Casley, DJ; Johnston, CI; Burrell, LM (May 2001). "In-vitro and in-vivo Inhibition of Rat Neutral Endopeptidase and Angiotensin Converting Enzyme with the Vasopeptidase Inhibitor Gemopatrilat". Journal of Hypertension. 19 (5): 941–6. doi:10.1097/00004872-200105000-00015. PMID 11393678.

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[INN-1] "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 46" (PDF). World Health Organization. p. 200. Retrieved 2 March 2017.

[2] "Gemopatrilat". AdisInsight. Highest Development Phases: Discontinued

[3] Laverman, GD; Van Goor, H; Henning, RH; De Jong, PE; De Zeeuw, D; Navis, G (January 2003). "Renoprotective Effects of VPI Versus ACEI in Normotensive Nephrotic Rats on Different Sodium Intakes". Kidney International. 63 (1): 64–71. doi:10.1046/j.1523-1755.2003.00708.x. PMID 12472769. Retrieved 2 March 2017.

[4] Wait, JC; Vaccharajani, N; Mitroka, J; Jemal, M; Khan, S; Bonacorsi, SJ; Rinehart, JK; Iyer, RA (June 2006). "Metabolism of [¹⁴C]Gemopatrilat After Oral Administration to Rats, Dogs, and Humans" (PDF). Drug Metabolism and Disposition. 34 (6): 961–70. doi:10.1124/dmd.105.007500. PMID 16540589. Retrieved 2 March 2017.

[5] Hubner, RA; Kubota, E; Casley, DJ; Johnston, CI; Burrell, LM (May 2001). "In-vitro and in-vivo Inhibition of Rat Neutral Endopeptidase and Angiotensin Converting Enzyme with the Vasopeptidase Inhibitor Gemopatrilat". Journal of Hypertension. 19 (5): 941–6. doi:10.1097/00004872-200105000-00015. PMID 11393678.

Antihypertensives: agents acting on the renin–angiotensin system (C09)
ACE inhibitors ("-pril")	Sulfhydryl-containing: Captopril Rentiapril Zofenopril Dicarboxylate-containing: Enalapril^# Benazepril Cilazapril Delapril Imidapril Lisinopril (+HCT) Moexipril Perindopril (+indapamide) Quinapril (+HCT) Ramipril Spirapril Temocapril Trandolapril Phosphonate-containing: Ceronapril Fosinopril (+HCT) Other/ungrouped: Alacepril
AIIRAs ("-sartan")	Azilsartan Candesartan Eprosartan Fimasartan Irbesartan Losartan (+HCT) Olmesartan (+amlodipine) Tasosartan^§ Telmisartan (+HCT) Valsartan (+HCT, +amlodipine)
Renin inhibitors ("-kiren")	Aliskiren (+amlodipine, +amlodipine and HCT) Remikiren^§
Dual ACE/NEP inhibitors	Gemopatrilat Ilepatril Omapatrilat Sampatrilat
Neprilysin inhibitors	Sacubitril (+valsartan)
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Angiotensin receptor modulators
ATR	Agonists: Angiotensin II Angiotensin III Angiotensin IV Saralasin Antagonists: Abitesartan Azilsartan Candesartan Elisartan Embusartan Eprosartan EXP-3174 Fimasartan Forasartan Irbesartan Losartan Milfasartan Olmesartan Olodanrigan PD123319 Pomisartan Pratosartan Ripisartan Saprisartan Sparsentan Tasosartan Telmisartan Valsartan Zolasartan ACE inhibitors: Alacepril Benazepril Captopril Cilazapril Delapril Enalapril Enalaprilat Fosinopril Gemopatrilat Imidapril Lisinopril Moexipril Omapatrilat Perindopril Quinapril Quinaprilat Ramipril Rentiapril Rescinnamine Spirapril Spiraprilat Temocapril Trandolapril Zofenopril Zofenoprilat Renin inhibitors: Aliskiren Ciprokiren Ditekiren Enalkiren Imarikiren Pepstatin Remikiren Terlakiren Zankiren Propeptides: Angiotensinogen Angiotensin I
Combinations:	Valsartan/hydrochlorothiazide Valsartan/hydrochlorothiazide/amlodipine Amlodipine/valsartan
See also Receptor/signaling modulators Signaling peptide/protein receptor modulators