bococizumab

{{Infobox drug

| type = mab

| image =

| alt =

| mab_type = mab

| source = zu/o

| target = Proprotein convertase subtilisin/kexin type 9 (PCSK9)

| tradename =

| Drugs.com =

| MedlinePlus =

| pregnancy_AU =

| pregnancy_US =

| pregnancy_category=

| legal_AU =

| legal_CA =

| legal_UK =

| legal_US =

| legal_status = Investigational

| routes_of_administration = Subcutaneous injection

| bioavailability =

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| CAS_number = 1407495-02-6

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 45M75JVK38

| ATC_prefix = none

| ATC_suffix =

| PubChemSubstance = 194168554

| DrugBank =

| IUPHAR_ligand = 7730

| ChEMBL = 3137349

| ChemSpiderID = none

| KEGG_Ref = {{keggcite|correct|kegg}}

| KEGG = D10621

| C=6414 | H=9918 | N=1722 | O=2012 | S=54

}}

Bococizumab (USAN;{{cite web|title=Statement On A Nonproprietary Name Adopted By The USAN Council: Bococizumab|publisher=American Medical Association|url=http://www.ama-assn.org/resources/doc/usan/x-pub/bococizumab.pdf}} development code RN316{{cite journal | author = World Health Organization | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 110 | journal = WHO Drug Information | volume = 27 | issue = 4 | year = 2013 | url =https://www.who.int/medicines/publications/druginformation/innlists/PL110.pdf | author-link = World Health Organization }}) is a drug that was in development by Pfizer targeting PCSK9 to reduce LDL cholesterol.{{cite news|title=Bococizumab (RN316) Significantly Reduced LDL Cholesterol In Statin-Treated Adults With High Cholesterol In A Phase 2b Study|url=http://press.pfizer.com/press-release/bococizumab-rn316-significantly-reduced-ldl-cholesterol-statin-treated-adults-high-cho|access-date=29 December 2014|archive-date=20 August 2019|archive-url=https://web.archive.org/web/20190820052746/https://press.pfizer.com/press-release/bococizumab-rn316-significantly-reduced-ldl-cholesterol-statin-treated-adults-high-cho|url-status=dead}} Pfizer withdrew the drug from development in November 2016, determining that it was "not likely to provide value to patients, physicians or shareholders."{{Cite news | url = https://www.reuters.com/article/us-pfizer-results-idUSKBN12W3S8 | date = Nov 1, 2016 | title = Pfizer scraps cholesterol fighter, trims profit forecast | publisher = Reuters}}

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.{{cite journal | vauthors = Weinreich M, Frishman WH | title = Antihyperlipidemic therapies targeting PCSK9 | journal = Cardiology in Review | volume = 22 | issue = 3 | pages = 140–6 | date = 2014 | pmid = 24407047 | doi = 10.1097/crd.0000000000000014 | s2cid = 2201087 }}

Clinical trials

A phase 2b study of statin patients was presented at the 2014 American College of Cardiology. 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. {{cite journal |last1=Ridker |first1=Paul |title=Lipid-Reduction Variability and AntidrugAntibody Formation with Bococizumab |journal=The New England Journal of Medicine |date=2017 |volume=376 |issue=16 |pages=1517–1526 |doi=10.1056/NEJMoa1614062 |pmid=28304227 |s2cid=205101298 |url=https://www.nejm.org/doi/full/10.1056/NEJMoa1614062 |access-date=24 September 2020|doi-access=free }} After assessing the data, Pfizer abandoned further development of bococizumab. {{cite web |last1=Adams |first1=Ben |title=Pfizer dumps PCSK9 inhibitor bococizumab after finding 'no value' in drug |url=https://www.fiercebiotech.com/biotech/pfizer-dumps-pcsk9i-inhibitor-bococizumab-after-finding-no-value-med |website=Fierce Biotech |date=November 2016 |publisher=Questex |access-date=24 September 2020}}

References

{{Monoclonals for bone, musculoskeletal, circulatory, and neurologic systems}}

Category:Hypolipidemic agents

Category:PCSK9 inhibitors

Category:Experimental monoclonal antibodies