Bococizumab Explained

Type:mab
Mab Type:mab
Source:zu/o
Target:Proprotein convertase subtilisin/kexin type 9 (PCSK9)
Legal Status:Investigational
Routes Of Administration:Subcutaneous injection
Cas Number:1407495-02-6
Unii:45M75JVK38
Atc Prefix:none
Pubchemsubstance:194168554
Iuphar Ligand:7730
Chembl:3137349
Chemspiderid:none
Kegg:D10621
C:6414
H:9918
N:1722
O:2012
S:54

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 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]

Notes and References

  1. Web site: Statement On A Nonproprietary Name Adopted By The USAN Council: Bococizumab. American Medical Association.
  2. World Health Organization . International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 110 . WHO Drug Information . 27 . 4 . 2013 . World Health Organization .
  3. News: Bococizumab (RN316) Significantly Reduced LDL Cholesterol In Statin-Treated Adults With High Cholesterol In A Phase 2b Study. 29 December 2014. 20 August 2019. https://web.archive.org/web/20190820052746/https://press.pfizer.com/press-release/bococizumab-rn316-significantly-reduced-ldl-cholesterol-statin-treated-adults-high-cho. dead.
  4. News: Pfizer scraps cholesterol fighter, trims profit forecast . Nov 1, 2016 . Reuters.
  5. Weinreich M, Frishman WH . Antihyperlipidemic therapies targeting PCSK9 . Cardiology in Review . 22 . 3 . 140–6 . 2014 . 24407047 . 10.1097/crd.0000000000000014 . 2201087 .
  6. Ridker . Paul . Lipid-Reduction Variability and AntidrugAntibody Formation with Bococizumab . The New England Journal of Medicine . 2017 . 376 . 16 . 1517–1526 . 10.1056/NEJMoa1614062 . 28304227 . 205101298 . 24 September 2020. free .
  7. Web site: Adams . Ben . Pfizer dumps PCSK9 inhibitor bococizumab after finding 'no value' in drug . Fierce Biotech . November 2016 . Questex . 24 September 2020.