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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^Y
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 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

^ "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).
^ ^a ^b "Bococizumab (RN316) Significantly Reduced LDL Cholesterol In Statin-Treated Adults With High Cholesterol In A Phase 2b Study". Archived from the original on 20 August 2019. 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. S2CID 2201087.
^ Ridker, Paul (2017). "Lipid-Reduction Variability and AntidrugAntibody Formation with Bococizumab". The New England Journal of Medicine. 376 (16): 1517–1526. doi:10.1056/NEJMoa1614062. PMID 28304227. S2CID 205101298. Retrieved 24 September 2020.
^ Adams, Ben (November 2016). "Pfizer dumps PCSK9 inhibitor bococizumab after finding 'no value' in drug". Fierce Biotech. Questex. Retrieved 24 September 2020.

Lipid-lowering agents (C10)

GI tract

Cholesterol absorption inhibitors, NPC1L1	Ezetimibe Hyzetimibe SCH-48461
Bile acid sequestrants/resins (LDL)	Colesevelam Colestilan Colestipol Colestyramine Colextran Soluble fiber such as psyllium and glucomannan

Liver

Statins (HMG-CoA reductase, LDL)	Atorvastatin Cerivastatin^‡ Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin^#
Niacin and derivatives (HDL and LDL)	Acipimox Aluminium nicotinate Niacin Niceritrol Nicofuranose Nicotinyl alcohol
MTTP inhibitors (VLDL)	Dirlotapide Lomitapide Mitratapide
ATP citrate lyase inhibitors (LDL)	Bempedoic acid
Thyromimetics (VLDL)	Dextrothyroxine^‡ Resmetirom

Blood vessels

PPAR agonists (LDL)

Fibrates	Aluminium clofibrate Bezafibrate Choline fenofibrate Ciprofibrate Clinofibrate Clofibrate^‡ Clofibride Etofibrate Fenofibrate Gemfibrozil Nafenopin Pemafibrate Ronifibrate Simfibrate
Others	GW501516^§

CETP inhibitors (HDL)

PCSK9 inhibitors (LDL)

ANGPTL3 inhibitors (LDL/HDL)

Evinacumab

Combinations

Other

Alipogene tiparvovec
Azacosterol
Azalanstat
Benfluorex^‡
Darapladib^§
Lapaquistat^§
Magnesium pyridoxal 5-phosphate glutamate
Meglutol
Mipomersen
Omega−3-acid ethyl esters
Policosanol
Probucol
Tiadenol
Triparanol^‡
Volanesorsen

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Monoclonals for bone, musculoskeletal, circulatory, and neurologic systems

Bone

Human	Burosumab Denosumab
Humanized	Blosozumab^† Romosozumab

Musculoskeletal

Human	Stamulumab^†

Circulatory

Human	Abelacimab Alirocumab Ascrinvacumab^§ Bentracimab^† Enoticumab Evinacumab Evolocumab Icrucumab Inclacumab Marstacimab Nesvacumab Orticumab Ramucirumab Rinucumab
Mouse	Biciromab^‡ Imciromab^‡
Chimeric	Abciximab Volociximab
Humanized	Alacizumab pegol Bevacizumab/Ranibizumab Bococizumab Brolucizumab Caplacizumab Concizumab Demcizumab Emicizumab Etaracizumab Faricimab Idarucizumab Ralpancizumab Tadocizumab Vanucizumab

Neurologic

Human	Anti-amyloid drugs Aducanumab^‡ Donanemab Gantenerumab^† Lecanemab Erenumab Fasinumab^† Fulranumab Opicinumab
Humanized	Bapineuzumab^† Crenezumab^† Eptinezumab Fremanezumab Galcanezumab Ozanezumab Ponezumab Refanezumab Semorinemab Solanezumab Tanezumab^†

Angiogenesis inhibitor

Humanized	Ranibizumab

Growth factor

Human	Bimagrumab Trevogrumab
Humanized	Domagrozumab Landogrozumab

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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