OnCo

A protein that stops cells from self-destructing. Venetoclax removes that protection and has transformed leukaemia treatment. This dossier gathers the 2 products (2 approved), 10 trials, 8 pathways and 0 resistance routes in the corpus that involve it, with external identifiers so it can be joined to UniProt, ChEMBL, Open Targets and the rest of biology.

Biology

Elsewhere: identifiers and databases

Built from HGNC, Ensembl, UniProt and ChEMBL ids

How common it is, by cancer

Full matrix →
CancerPrevalenceSource
Chronic lymphocytic leukaemia
>90%
Wikipedia
Diffuse large B-cell lymphoma
30-40%
Wikipedia
Acute myeloid leukaemia
n/a
Wikipedia

Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.

Mutation hotspots and which drugs address them

BH4BH1Transmembrane160120179239BCL2 residue (239 aa, P10415)G101VD103Y / F104L
ResistanceLarger dot: a product in the corpus addresses the residue.
ResidueKindWhat it doesAddressed by
G101V
101
ResistanceReduces venetoclax affinity about 180-fold; found in a subset of CLL relapsing on continuous venetoclax, often subclonal. Sonrotoclax is reported to retain activity against it.
D103Y / F104L
103
ResistanceAdditional BH3-groove mutations co-occurring with G101V.

Frequencies are quoted from the source on each row; a blank means no figure was sourced, not that it is rare. Domain boundaries are approximate. Sources for the map: COSMIC: BCL2.

Products by modality and phase

Browse products →
ModalityApproved
Small molecule
2
TrialPhaseStatus
AMPLIFY
NCT03836261
3Positive
CLL13 / GAIA
NCT02950051
3Positive
SEQUOIA
NCT03336333
3Positive
GLOW
NCT03462719
3Positive
VIALE-A
NCT02993523
3Positive
CLL14
NCT02242942
3Positive
CELESTIAL-TNCLL
NCT06073821
3Active
myeloMATCH
NCT05564390
platformRecruiting
ASCERTAIN-V
NCT04657081
2Positive
CAPTIVATE
NCT02910583
2Positive

Resistance routes that involve this target

Unaddressed routes →

The resistance atlas has no route that names this target.

Pathways where it is a node

Pathway-to-drug matrix →
  • B-cell receptor / BTK signalling (to NF-κB)
    Node: BCL2, IL-6, IL-10, cyclin D → survival · 1 druggable nodes

    The B-cell receptor is the survival switch of B cells. Signals from it pass through BTK to free NF-kappa-B, which keeps the cell alive. B-cell cancers hold it on; BTK inhibitors, proteasome inhibitors and lenalidomide each cut the line at a different point.

    Which nodes have drugs →
  • Drug-tolerant persister cells
    Node: Efflux, autophagy, BCL-XL · 3 druggable nodes

    Even when a drug wipes out 99% of a tumour, a few cells survive without any resistance mutation: they go quiet, stop dividing, and wait. These persisters are the seed of relapse. They are hard to kill precisely because they are not doing much, but they have their own weaknesses.

    Which nodes have drugs →
  • Extrinsic apoptosis (death receptors)
    Node: tBID → mitochondria · 2 druggable nodes

    Immune cells kill by touch: they present FAS ligand or TRAIL to a target cell, whose death receptors then trigger self-destruction from the outside in. Tumours cut this wire by deleting the receptors or over-producing decoys and blockers.

    Which nodes have drugs →
  • Ferroptosis & regulated cell death
    Node: Apoptosis (BCL-2 family) · 1 druggable nodes

    Cells can die in several programmed ways. Beyond the classic apoptosis, ferroptosis kills through iron-driven fat oxidation, and drug-resistant, mesenchymal cancer cells turn out to be unusually prone to it.

    Which nodes have drugs →
  • Intrinsic apoptosis (BCL-2 family)
    Node: BCL-2 / BCL-XL / MCL-1 · 1 druggable nodes

    Intrinsic apoptosis is the cell's self-destruct switch. BCL-2 holds it shut; BAX and BAK pull it open. Venetoclax pries BCL-2 off so the switch can fire.

    Which nodes have drugs →
  • Mitosis & the spindle assembly checkpoint
    Node: Mitotic death (BCL-XL↓) · 3 druggable nodes

    When a cell divides, a scaffold of microtubules (the spindle) pulls one copy of each chromosome to each side. A checkpoint holds the split until every chromosome is hooked on. Taxanes and vinca alkaloids freeze the spindle so the cell is stuck at this checkpoint until it dies.

    Which nodes have drugs →
  • The p53 network (guardian of the genome)
    Node: PUMA, NOXA → apoptosis · 4 druggable nodes

    p53 is the cell's emergency coordinator. Damage, oncogene stress, or lack of oxygen switch it on; it then pauses division, orders repairs, or triggers suicide or permanent retirement. MDM2 keeps it switched off in healthy cells. Half of all cancers break p53 outright; many of the rest over-produce MDM2.

    Which nodes have drugs →
  • Transcriptional machinery & addiction
    Node: MYC, MCL-1 (short-lived) · 4 druggable nodes

    Cancer cells run a few genes (MYC, their lineage factors, their fusion oncogenes) at extreme volume from giant control regions called super-enhancers. The amplifiers, BRD4, CDK7, CDK9 and Mediator, are the same in every cell, but cancers are unusually dependent on them, and that dependence is druggable.

    Which nodes have drugs →

Companion diagnostics and assays

Assay registry →

No companion diagnostic in the registry measures this target.

Preclinical models

All models →

No model entry for this target yet; check the cancer entries on the models page.

  1. 01

    Is fixed-duration venetoclax-based therapy curative for a subset of CLL, and who needs retreatment?

    clinicalclinic

    Why unresolved. CLL14 and AMPLIFY show long treatment-free remissions after one or two years; measurable-residual-disease kinetics predict relapse but retreatment strategies and the role of newer BCL2 inhibitors are unsettled.

    What would answer it. Long-term follow-up with MRD-guided retreatment trials and comparison of sonrotoclax with venetoclax.

    Source: CLL14, NEJM 2019

Ideas and companies

Key papers and the live literature

Preprints →
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this target: (TITLE:"BCL-2" OR ABSTRACT:"BCL-2" OR TITLE:"BCL2" OR ABSTRACT:"BCL2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about BCL-2, not a curated reading list.

Export

The dossier as machine-readable JSON: identifiers from HGNC, Ensembl, UniProt and ChEMBL, products with status, trials, pathways, hotspots, open questions and assays. The full entity record is in the open API at /api/v1/entities/bcl2.json. Licence CC BY 4.0.