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

General Information of Drug (ID: DMVGMNC)

• Drug Name: MK-0616 Drug Info
• Synonyms: MK0616; MK-0616; GTPL12689; GLXC-27059; PCSK9 macrocyclic peptide inhibitor MK-0616

Indication

Disease Entry	ICD 11	Status	REF
Hypercholesterolaemia	5C80.0	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 167312471
  TTD Drug ID: DMVGMNC

Molecule-Related Drug Atlas

Drug(s) Targeting Proprotein convertase subtilisin/kexin type 9 (PCSK9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
REGN-727	DM87XSN	Familial hypercholesterolemia	5C80.00	Approved	[3]
Evolocumab	DMNSAND	Heterozygous familial hypercholesterolemia	5C80.00	Approved	[4]
Bococizumab	DM2OBNW	Chronic obstructive pulmonary disease	CA22	Phase 3	[5]
PF-04950615	DM0TWCY	Hypercholesterolaemia	5C80.0	Phase 3	[6]
AMG 145	DMG324Y	Hypercholesterolaemia	5C80.0	Phase 3	[7]
LIB003	DMVP8WU	Hypercholesterolaemia	5C80.0	Phase 3	[8]
LY3015014	DMFMKQ3	Cardiovascular disease	BA00-BE2Z	Phase 2	[5]
PCSK9 Adnectin	DMH86KO	Cardiovascular disease	BA00-BE2Z	Phase 1	[9]
SPC5001	DMUPQ70	Hyperlipidaemia	5C80	Phase 1	[10]
AZD0780	DMAFPNI	Elevated Lipoprotein(a)	5C80.1	Phase 1	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proprotein convertase subtilisin/kexin type 9 (PCSK9)	TTBRG7E	PCSK9_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT05261126) A Phase 2b, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of MK-0616 in Adults With Hypercholesterolemia. U.S.National Institutes of Health.
• [2] Phase 2b Randomized Trial of the Oral PCSK9 Inhibitor MK-0616. J Am Coll Cardiol. 2023 Apr 25;81(16):1553-1564.
• [3] Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce low-density lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a phase 2 randomised controlled trial. Lancet. 2012 Jul 7;380(9836):29-36.
• [4] Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease. N Engl J Med. 2017 May 4;376(18):1713-1722.
• [5] The dyslipidaemia market. Nat Rev Drug Discov. 2014 Nov;13(11):807-8.
• [6] Phase 3 data for PCSK9 inhibitor wows. Nat Biotechnol. 2013 Dec;31(12):1057-8.
• [7] PCSK9 inhibition with evolocumab (AMG 145) in heterozygous familial hypercholesterolaemia (RUTHERFORD-2): a randomised, double-blind, placebo-controlled trial. Lancet. 2015 Jan 24;385(9965):331-40.
• [8] ClinicalTrials.gov (NCT05234775) Cross-Over Study to Compare the Pharmacokinetics and Pharmacodynamics of LIB003 Process 1 and Process 2 Drug Product in Subjects With or Without Statin Therapy. U.S.National Institutes of Health.
• [9] Pharmacologic profile of the Adnectin BMS-962476, a small protein biologic alternative to PCSK9 antibodies for low-density lipoprotein lowering. J Pharmacol Exp Ther. 2014 Aug;350(2):412-24.
• [10] 2011 Pipeline of Santaris Pharma.
• [11] Clinical pipeline report, company report or official report of AstraZeneca