Tafolecimab

Summary

Tafolecimab (CHEMBL4594554) is a phase-3 clinical-stage antibody targeting PCSK9; indicated across 4 conditions including familial hypercholesterolemia and lung neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Antibody
• Targets: 1 (PCSK9)
• Indications: 4 conditions
• Clinical trials: 13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4594554
Name	Tafolecimab
Type	Antibody
Max phase	3

Also known as: IBI-306, Ibi306, IBI306, Tafolecimab, TAFOLECIMAB

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		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
familial hypercholesterolemia	3	MONDO:0005439	EFO:0004911
lung neoplasm	2	MONDO:0021117	MONDO:0008903

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

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE2	4
PHASE3	3
PHASE2/PHASE3	2
Not specified	2
PHASE4	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06683131	PHASE4	NOT_YET_RECRUITING	Effectiveness of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor Initiation Before Percutaneous Coronary Intervention on Acute Myocardial Infarction Patients
NCT07473960	PHASE3	RECRUITING	IBI306 Monotherapy in Non-Familial Hypercholesterolemia and Mixed Hyperlipidemia
NCT04031742	PHASE2/PHASE3	COMPLETED	A Study to Evaluate Safety and Efficacy of IBI306, a PCSK9 Monoclonal Antibody in Chinese Subjects With Homozygous Familial Hypercholesterolemia
NCT04179669	PHASE3	COMPLETED	Safety and Efficacy of IBI306 in HeFH Patients
NCT04709536	PHASE3	COMPLETED	A Study of IBI306 in Participants With Hypercholesterolemia
NCT04948008	PHASE2/PHASE3	UNKNOWN	Evaluate the Efficacy and Safety of IBI306 in Subjects With Homozygous Familial Hypercholesterolemia
NCT06421298	PHASE2	RECRUITING	A Prospective, Single-arm, Phase II Clinical Trial to Evaluate the Efficacy and Safety of Tafolecimab and Sintilimab Combined With Chemotherapy in Patients With Advanced or Metastatic Driver Gene-negative Non-small Cell Lung Cancer After Failure of First-line Immunotherapy.
NCT07014215	PHASE2	NOT_YET_RECRUITING	PD-1 Combined With Bevacizumab and PCSK-9 Inhibitor in Patients With Advanced NSCLC Who Have Progressed After Anti- PD- 1/L1 Therapy
NCT07061535	PHASE2	NOT_YET_RECRUITING	Sintilimab Combined With Tafolecimab and Chemotherapy as First-Line Treatment for Extensive-Stage Small Cell Lung Cancer
NCT03815812	PHASE2	COMPLETED	Multiple Ascending Dose Study of PCSK-9 Inhibitor (IBI306) in Chinese Patients With Hypercholesterolemia
NCT03366688	PHASE1	COMPLETED	Single Ascending Dose Study of PCSK-9 Inhibitor (IBI306) in Healthy Subjects.
NCT06096909	Not specified	NOT_YET_RECRUITING	Early Initiation of Tafolecimab for Patients With Acute Coronary Syndromeundergoing Percutaneous Coronary Intervention in Chinese Population
NCT07341958	Not specified	NOT_YET_RECRUITING	INtensive liPid-lowering Therapy for Acute High-risk IntracRanial or Extracranial atheroSclerosis -II (INSPIRES-2)

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