Bococizumab

Bococizumab
Monoclonal antibody
Type	Whole antibody
Source	Humanized (from mouse)
Target	Proprotein convertase subtilisin/kexin type 9 (PCSK9)
Clinical data
Routes of; administration	Subcutaneous injection
ATC code	none;
Legal status
Legal status	Investigational;
Identifiers
CAS Number	1407495-02-6;
PubChem SID	194168554;
IUPHAR/BPS	7730;
ChemSpider	none;
UNII	45M75JVK38;
KEGG	D10621 ;
ChEMBL	ChEMBL3137349;
Chemical and physical data
Formula	C6414H9918N1722O2012S54
Molar mass	145077.18 g·mol−1

Bococizumab (USAN;[1] development code RN316[2]) is a drug that was in development by Pfizer targeting PCSK9 to reduce LDL cholesterol.[3] Pfizer withdrew the drug from development in November 2016, determining that it was "not likely to provide value to patients, physicians or shareholders."[4]

Description

Bococizumab is a monoclonal antibody that inhibits PCSK9, a protein that interferes with the removal of LDL. LDL levels are a major risk factor for cardiovascular disease.[5]

Clinical trials

A phase 2b study of statin patients was presented at the 2014 American College of Cardiology.[3] Monthly or bimonthly injections resulted in significantly reduced LDL-C at week 12.

The Phase 3 SPIRE trials plan to enroll 17,000 patients to measure cardiovascular risk. High risk and statin intolerant subjects will be included.

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References

"Statement On A Nonproprietary Name Adopted By The USAN Council: Bococizumab" (PDF). American Medical Association.
World Health Organization (2013). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 110" (PDF). WHO Drug Information. 27 (4).
"Bococizumab (RN316) Significantly Reduced LDL Cholesterol In Statin-Treated Adults With High Cholesterol In A Phase 2b Study". Retrieved 29 December 2014.
"Pfizer scraps cholesterol fighter, trims profit forecast". Reuters. Nov 1, 2016.
Weinreich M, Frishman WH (2014). "Antihyperlipidemic therapies targeting PCSK9". Cardiology in Review. 22 (3): 140–6. doi:10.1097/crd.0000000000000014. PMID 24407047.

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[1] "Statement On A Nonproprietary Name Adopted By The USAN Council: Bococizumab" (PDF). American Medical Association.

[2] World Health Organization (2013). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 110" (PDF). WHO Drug Information. 27 (4).

[pfizer-3] "Bococizumab (RN316) Significantly Reduced LDL Cholesterol In Statin-Treated Adults With High Cholesterol In A Phase 2b Study". Retrieved 29 December 2014.

[4] "Pfizer scraps cholesterol fighter, trims profit forecast". Reuters. Nov 1, 2016.

[5] Weinreich M, Frishman WH (2014). "Antihyperlipidemic therapies targeting PCSK9". Cardiology in Review. 22 (3): 140–6. doi:10.1097/crd.0000000000000014. PMID 24407047.