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

General Information of Drug (ID: DMQ1LWU)

• Drug Name: M-100240 Drug Info
• Synonyms: Mdl 100240; M100,240; MDL-100240; Mdl 100,142; Mdl 100,240; (4S,7S,12bR)-7-[[(2S)-2-acetylsulfanyl-3-phenylpropanoyl]amino]-6-oxo-2,3,4,7,8,12b-hexahydro-1H-pyrido[2,1-a][2]benzazepine-4-carboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Hypotension	BA20-BA21	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 133985
  CAS Number: CAS 142695-08-7
  TTD Drug ID: DMQ1LWU

Molecule-Related Drug Atlas

Drug(s) Targeting Neutral endopeptidase (MME)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LCZ696	DMLFX7K	Heart failure	BD10-BD13	Approved	[3]
Candoxatril	DMHJCGV	Hypertension	BA00-BA04	Phase 3	[4]
Gallopamil	DMXBR27	Asthma	CA23	Phase 2	[5]
SLV 306	DMCDON3	Acute decompensated heart failure	BD1Z	Phase 2	[6]
SLV-334	DMXCJKY	Brain injury	NA07.Z	Phase 2	[7]
VX-15	DMLWM4G	Huntington disease	8A01.10	Phase 2	[8]
Sampatrilat	DMXTOVE	Hypotension	BA20-BA21	Phase 2	[9]
SLV-338	DM7WKTM	Cardiovascular disease	BA00-BE2Z	Phase 1	[10]
GW-796406	DMQ46DN	Hypotension	BA20-BA21	Phase 1	[5]
Debio 0827	DMQIEFB	Chronic pain	MG30	Phase 1	[11]

Drug(s) Targeting Angiotensin-converting enzyme (ACE)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enalapril	DMNFUZR	Congestive heart failure	BD10	Approved	[12]
Spirapril	DM5XLTY	Hypertension	BA00-BA04	Approved	[13]
Captopril	DM458UM	Chronic heart failure	BD1Z	Approved	[14]
Benazepril	DMH1M9B	Hypertension	BA00-BA04	Approved	[15]
Moexipril	DM26E4B	Hypertension	BA00-BA04	Approved	[16]
Ramipril	DM2R68E	Acute heart failure	BD10-BD13	Approved	[17]
Perindopril	DMOPZDT	Hypertension	BA00-BA04	Approved	[18]
Trandolapril	DM4L6EU	Chronic heart failure	BD1Z	Approved	[19]
Fosinopril	DM9NJ52	Chronic heart failure	BD1Z	Approved	[20]
Lisinopril	DMUOK4C	Chronic heart failure	BD1Z	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin-converting enzyme (ACE)	TTL69WB	ACE_HUMAN	Modulator	[2]
Neutral endopeptidase (MME)	TT5TKPM	NEP_HUMAN	Modulator	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002832)
• [2] Effects of MDL 100,240, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase on the vasopressor response to exogenous angiot... J Cardiovasc Pharmacol. 1998 Mar;31(3):408-17.
• [3] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [4] Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model. Indian Pacing Electrophysiol J. 2008 Apr 1;8(2):102-13.
• [5] Mechanism of vasopeptidase inhibitor-induced plasma extravasation: comparison of omapatrilat and the novel neutral endopeptidase 24.11/angiotensin-converting enzyme inhibitor GW796406. J Pharmacol Exp Ther. 2005 Dec;315(3):1306-13.
• [6] The dual endothelin converting enzyme/neutral endopeptidase inhibitor SLV-306 (daglutril), inhibits systemic conversion of big endothelin-1 in humans. Life Sci. 2012 Oct 15;91(13-14):743-8.
• [7] Clinical trials in traumatic brain injury: past experience and current developments.Neurotherapeutics.2010 Jan;7(1):115-26.
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Sustained antihypertensive actions of a dual angiotensin-converting enzyme neutral endopeptidase inhibitor, sampatrilat, in black hypertensive subjects. Am J Hypertens. 1999 Jun;12(6):563-71.
• [10] Renoprotective effects of combined endothelin-converting enzyme/neutral endopeptidase inhibitor SLV338 in acute and chronic experimental renal damage. Clin Lab. 2011;57(7-8):507-15.
• [11] Clinical pipeline report, company report or official report of Debiopharm (2011).
• [12] Determination of bezafibrate, methotrexate, cyclophosphamide, orlistat and enalapril in waste and surface waters using on-line solid-phase extracti... J Environ Monit. 2009 Apr;11(4):830-8.
• [13] Central angiotensin II controls alcohol consumption via its AT1 receptor. FASEB J. 2005 Sep;19(11):1474-81.
• [14] Using ACE inhibitors appropriately. Am Fam Physician. 2002 Aug 1;66(3):461-8.
• [15] Efficacy of benazepril hydrochloride to delay the progression of occult dilated cardiomyopathy in Doberman Pinschers. J Vet Intern Med. 2009 Sep-Oct;23(5):977-83.
• [16] Moexipril for treatment of primary biliary cirrhosis in patients with an incomplete response to ursodeoxycholic acid. Dig Dis Sci. 2010 Feb;55(2):476-83.
• [17] Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
• [18] Fixed combination perindopril-amlodipine (Coveram) in the treatment of hypertension and coronary heart disease. Rev Med Liege. 2009 Apr;64(4):223-7.
• [19] Selective reduction of central pulse pressure under angiotensin blockage in SHR: role of the fibronectin-alpha5beta1 integrin complex. Am J Hypertens. 2009 Jul;22(7):711-7.
• [20] Angiotensin-converting enzyme inhibition and novel cardiovascular risk biomarkers: results from the Trial of Angiotensin Converting Enzyme Inhibition and Novel Cardiovascular Risk Factors (TRAIN) study. Am Heart J. 2009 Feb;157(2):334.e1-8.
• [21] Involvement of vascular angiotensin II-forming enzymes in the progression of aortic abdominal aneurysms in angiotensin II- infused ApoE-deficient m... J Atheroscler Thromb. 2009 Jun;16(3):164-71.