Bococizumab

Summary

Bococizumab (CHEMBL3137349) is a phase-3 clinical-stage antibody targeting PCSK9; indicated across 4 conditions including cardiovascular disorder and familial hypercholesterolemia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Antibody
• Targets: 1 (PCSK9)
• Indications: 4 conditions
• Clinical trials: 20

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3137349
Name	Bococizumab
Type	Antibody
Max phase	3

Also known as: Bococizumab, PF-04950615, RN-316, RN316, BOCOCIZUMAB

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PCSK9	proprotein convertase subtilisin/kexin type 9	Binding	10	4.6%	Q8NBP7

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): PCSK9.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)	1	PCSK9
VLDLR internalisation and degradation	1	PCSK9
Post-translational protein phosphorylation	1	PCSK9
LDL clearance	1	PCSK9

Dominant GO biological processes

GO term	Targets
kidney development	1
liver development	1
negative regulation of receptor recycling	1
negative regulation of receptor internalization	1
positive regulation of receptor internalization	1
triglyceride metabolic process	1
phospholipid metabolic process	1
apoptotic process	1
lysosomal transport	1
cholesterol metabolic process	1
cellular response to starvation	1
negative regulation of low-density lipoprotein particle clearance	1
protein autoprocessing	1
neurogenesis	1
neuron differentiation	1

Indications & clinical

Indications

4 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	3	MONDO:0004995	EFO:0000319
familial hypercholesterolemia	3	MONDO:0005439	EFO:0004911
hyperlipidemia	3	MONDO:0021187	MONDO:0021187

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 20.

Phase distribution

Phase	Trials
PHASE3	10
PHASE1	6
PHASE2	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01968954	PHASE3	COMPLETED	Randomized Clinical Trial Of Bococizumab (PF-04950615; RN316) In Subjects With Hyperlipidemia Or Mixed Dyslipidemia At Risk Of Cardiovascular Events
NCT01968967	PHASE3	COMPLETED	Randomized Clinical Trial of Bococizumab (PF-04950615; RN316) in Subjects With Hyperlipidemia or Mixed Dyslipidemia at Risk of Cardiovascular Events
NCT01968980	PHASE3	COMPLETED	A 52 Week Study To Assess The Use Of Bococizumab (PF-04950615; RN316) In Subjects With Heterozygous Familial Hypercholesterolemia
NCT01975376	PHASE3	TERMINATED	The Evaluation of Bococizumab (PF-04950615;RN316) in Reducing the Occurrence of Major Cardiovascular Events in High Risk Subjects
NCT01975389	PHASE3	TERMINATED	The Evaluation of Bococizumab (PF-04950615; RN316) in Reducing the Occurrence of Major Cardiovascular Events in High Risk Subjects
NCT02100514	PHASE3	COMPLETED	Randomized Clinical Trial of Bococizumab (PF-04950615; RN316) in Subjects With Primary Hyperlipidemia or Mixed Dyslipidemia At Risk Of Cardiovascular Events
NCT02135029	PHASE3	COMPLETED	Randomized Clinical Trial of Bococizumab (PF-04950615; RN316) in Subjects Who Are Intolerant to Statins
NCT02458287	PHASE3	COMPLETED	Efficacy, Safety, Tolerability And Actual Use Study Of Bococizumab And An Autoinjector (Pre-Filled Pen) In Subjects With Hyperlipidemia Or Dyslipidemia
NCT02524106	PHASE3	TERMINATED	Bococizumab HIV Evaluation (B-HIVE) Study
NCT02947334	PHASE3	WITHDRAWN	Efficacy And Safety Of Bococizumab For Lipid Lowering In Asian Hypercholesterolemia Subjects
NCT01342211	PHASE2	COMPLETED	A Multiple Dose Study of PF-04950615 (RN316) in Subjects on High Doses of Statins
NCT01350141	PHASE2	COMPLETED	A Multiple Dose Study Of PF-04950615 (RN316) In Subjects On Maximum Doses Of Statins
NCT01592240	PHASE2	COMPLETED	Monthly And Twice Monthly Subcutaneous Dosing Of PF-04950615 (RN316) In Hypercholesterolemic Subjects On A Statin
NCT02055976	PHASE2	COMPLETED	Dose Ranging Study Of Bococizumab (PF-04950615; RN316) In Hypercholesterolemic Japanese Subjects
NCT00991159	PHASE1	COMPLETED	A Study To Access The Safety And Tolerability Of RN316 (PF-04950615) When Administered To Healthy Adult Subjects
NCT01243151	PHASE1	COMPLETED	Safety And Tolerability Of Multiple Doses Of PF-04950615 (RN316) In Subjects With Hypercholesterolemia
NCT01435382	PHASE1	COMPLETED	A Pharmacokinetic and Pharmacodynamic Study of PF-04950615 (RN316) in Subjects With Hypercholesterolemia
NCT01720537	PHASE1	COMPLETED	A Study To Assess The Safety Of PF-05335810 In Hypercholesterolemic Subjects
NCT02043301	PHASE1	COMPLETED	Pharmacokinetics And Relative Bioavailability Of Bococizumab (PF-04950615; RN316) When Administered To The Abdomen, Thigh Or Upper Arm
NCT02458209	PHASE1	COMPLETED	Single Dose Manufacturing Site (Pfizer vs. BIP) And Device (Prefilled Syringe vs. Prefilled Pen) Comparability Study For Bococizumab In Healthy Volunteers

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

1 molecules share ≥1 primary target. Top 1 by shared-target count:

Molecule	Source	Status	Shared targets
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	PCSK9