Bococizumab

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]

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
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC6414H9918N1722O2012S54
Molar mass145077.18 g·mol−1

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 were dose-finding studies and found bococizumab to significantly reduce LDL cholesterol levels, but was commonly associated with anti-drug antibodies. The development of anti-drug antibodies with bococizumab led to an attenuation in LDL lowering at 52 weeks. Wide variation in the relative reduction in cholesterol levels was additionally observed among those not developing antidrug antibodies. [6] After assessing the data, Pfizer abandoned further development of bococizumab. [7]

References
  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. "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. S2CID 2201087.
  6. Ridker, Paul (2017). "Lipid-Reduction Variability and AntidrugAntibody Formation with Bococizumab". The New England Journal of Medicine. 376 (16): 1517. doi:10.1056/NEJMoa1614062. PMID 28304227. Retrieved 24 September 2020.
  7. Adams, Ben. "Pfizer dumps PCSK9 inhibitor bococizumab after finding 'no value' in drug". Fierce Biotech. Questex. Retrieved 24 September 2020.
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