Tigatuzumab
drugOn this page
Also known as Anti-dr5 moabAnti-trail-r2 moabCS-1008TRA-8
Summary
Tigatuzumab (CHEMBL1743080) is a phase-3 clinical-stage antibody targeting TNFRSF10B; indicated across 8 conditions including hepatocellular carcinoma and exocrine pancreatic carcinoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Antibody
- Targets: 1 (TNFRSF10B)
- Indications: 8 conditions
- Clinical trials: 7
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1743080 |
| Name | Tigatuzumab |
| Type | Antibody |
| Max phase | 3 |
Also known as: Anti-dr5 moab, Anti-trail-r2 moab, CS-1008, Tigatuzumab, TRA-8, TIGATUZUMAB
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 |
|---|---|---|---|---|---|
| TNFRSF10B | death receptor 5 | Agonist | 8.52 | 0% | O14763 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): TNFRSF10B.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Caspase activation via Death Receptors in the presence of ligand | 1 | TNFRSF10B |
| Cell surface interactions at the vascular wall | 1 | TNFRSF10B |
| Regulation by c-FLIP | 1 | TNFRSF10B |
| RIPK1-mediated regulated necrosis | 1 | TNFRSF10B |
| CASP8 activity is inhibited | 1 | TNFRSF10B |
| TP53 Regulates Transcription of Death Receptors and Ligands | 1 | TNFRSF10B |
| Dimerization of procaspase-8 | 1 | TNFRSF10B |
| TRAIL signaling | 1 | TNFRSF10B |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| defense response to tumor cell | 1 |
| apoptotic process | 1 |
| cell surface receptor signaling pathway | 1 |
| activation of NF-kappaB-inducing kinase activity | 1 |
| extrinsic apoptotic signaling pathway via death domain receptors | 1 |
| response to endoplasmic reticulum stress | 1 |
| TRAIL-activated apoptotic signaling pathway | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of apoptotic process | 1 |
| positive regulation of canonical NF-kappaB signal transduction | 1 |
| intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress | 1 |
| cellular response to mechanical stimulus | 1 |
| signal transduction | 1 |
Indications & clinical
Indications
8 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 |
|---|---|---|---|
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| colorectal neoplasm | 1 | MONDO:0005335 | EFO:0004142 |
| neoplasm | 1 | MONDO:0005070 | MONDO:0004992 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 5 |
| PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00945191 | PHASE2 | COMPLETED | Combination Chemotherapy With CS-1008 to Treat Ovarian Cancer |
| NCT00969033 | PHASE2 | TERMINATED | CS-1008 Used With Irinotecan Versus Irinotecan Alone in Subjects With Metastatic Colorectal Carcinoma Who Failed First-line Treatment With Oxaliplatin |
| NCT00991796 | PHASE2 | COMPLETED | CS-1008 With Carboplatin/Paclitaxel in Chemotherapy naïve Subjects With Metastatic or Unresectable Non-small Cell Lung Cancer (NSCLC) |
| NCT01033240 | PHASE2 | COMPLETED | CS1008- in Combination With Sorafenib Compared to Sorafenib Alone in Subjects With Advanced Liver Cancer |
| NCT01307891 | PHASE2 | COMPLETED | Abraxane With or Without Tigatuzumab in Patients With Metastatic, Triple Negative Breast Cancer |
| NCT01124630 | PHASE1 | COMPLETED | Study of CS-1008 in Combination With FOLFIRI in Patients Who Have Failed Other Treatments |
| NCT01220999 | PHASE1 | COMPLETED | A Phase I Imaging and Pharmacodynamic Trial of CS-1008 in Patients With Metastatic Colorectal Cancer |
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
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Genes: TNFRSF10B