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;
KEGG	D10621 ;
ChEMBL	ChEMBL3137349;
Chemical and physical data
Formula	C6414H9918N1722O2012S54
Molar mass	145.1 kg/mol 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.

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.