Bococizumab

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Bococizumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from mouse)
TargetProprotein convertase subtilisin/kexin type 9 (PCSK9)
Clinical data
Routes of
administration
Subcutaneous injection
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem SID
IUPHAR/BPS
ChemSpider
  • none
KEGG
ChEMBL
Chemical and physical data
FormulaC6414H9918N1722O2012S54
Molar mass145.1 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[edit]

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[edit]

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.[needs update] High risk and statin intolerant subjects will be included.[needs update]

References[edit]

  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).
  3. ^ a b "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.