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

General Information of DTT (ID: TTBRG7E)

• DTT Name: Proprotein convertase subtilisin/kexin type 9 (PCSK9) DTT Info
• Gene Name: PCSK9

Molecule-Related Drug & Molecule List

2 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Evolocumab	DMNSAND	Heterozygous familial hypercholesterolemia	5C80.00	Approved	[1]
REGN-727	DM87XSN	Familial hypercholesterolemia	5C80.00	Approved	[2]

10 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMG 145	DMG324Y	Hypercholesterolaemia	5C80.0	Phase 3	[3]
Bococizumab	DM2OBNW	Chronic obstructive pulmonary disease	CA22	Phase 3	[4]
LIB003	DMVP8WU	Hypercholesterolaemia	5C80.0	Phase 3	[5]
PF-04950615	DM0TWCY	Hypercholesterolaemia	5C80.0	Phase 3	[6]
LY3015014	DMFMKQ3	Cardiovascular disease	BA00-BE2Z	Phase 2	[4]
MK-0616	DMVGMNC	Hypercholesterolaemia	5C80.0	Phase 2	[7]
AZD0780	DMAFPNI	Elevated Lipoprotein(a)	5C80.1	Phase 1	[8]
NNC-0385-0434	DMBII8C	Hypercholesterolaemia	5C80.0	Phase 1	[9]
PCSK9 Adnectin	DMH86KO	Cardiovascular disease	BA00-BE2Z	Phase 1	[10]
SPC5001	DMUPQ70	Hyperlipidaemia	5C80	Phase 1	[11]

1 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1D05	DMGSQTK	Coronary artery disease	BA80	Investigative	[12]

References

• [1] Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease. N Engl J Med. 2017 May 4;376(18):1713-1722.
• [2] 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.
• [3] 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.
• [4] The dyslipidaemia market. Nat Rev Drug Discov. 2014 Nov;13(11):807-8.
• [5] 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.
• [6] Phase 3 data for PCSK9 inhibitor wows. Nat Biotechnol. 2013 Dec;31(12):1057-8.
• [7] Phase 2b Randomized Trial of the Oral PCSK9 Inhibitor MK-0616. J Am Coll Cardiol. 2023 Apr 25;81(16):1553-1564.
• [8] Clinical pipeline report, company report or official report of AstraZeneca
• [9] ClinicalTrials.gov (NCT04058834) A First Human Dose Trial Investigating Safety, Tolerability and Pharmacokinetics of Single Doses of NNC0385-0434 in Healthy Subjects and Patients With Hypercholesterolaemia. U.S.National Institutes of Health.
• [10] 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.
• [11] 2011 Pipeline of Santaris Pharma.
• [12] A PCSK9-binding antibody that structurally mimics the EGF(A) domain of LDL-receptor reduces LDL cholesterol in vivo. J Lipid Res. 2011 Jan;52(1):78-86.