Vemurafenib
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Also known as PLX-4032PLX4032RG 7204RG-7204RO 5185426RO-5185426ZelborafSID137275900VermurafenibVemurafenibVemurafenibÊVemurafenibÂ
Summary
Vemurafenib (CHEMBL1229517) is an approved small-molecule antineoplastic agent (ATC L01EC01) targeting BRAF and RAF1; indicated across 22 conditions including melanoma and metastatic melanoma; with CIViC clinical evidence for 186 variant-indication associations (e.g. BRAF V600 in melanoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EC01
- Targets: 2 (BRAF, RAF1)
- Indications: 22 conditions
- Clinical trials: 132
- Precision-oncology evidence (CIViC): 186 variant–indication associations
- Chemistry: 489.9 Da · C23H18ClF2N3O3S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1229517 |
| Name | Vemurafenib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 42611257 |
| ChEBI | CHEBI:63637 |
| ATC | L01EC01 |
| Molecular formula | C23H18ClF2N3O3S |
| Molecular weight | 489.9 |
| InChIKey | GPXBXXGIAQBQNI-UHFFFAOYSA-N |
SMILES: CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)Cl)F
IUPAC name: N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
ChEBI definition: A pyrrolopyridine that is 1H-pyrrolo[2,3-b]pyridine which is substituted at position 5 by a p-chlorophenyl group and at positions 3 by a 3-amino-2,6-difluorobenzoyl group, the amino group of which has undergone formal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases.
Pharmacological roles (ChEBI): antineoplastic agent, B-Raf inhibitor.
Also known as: PLX-4032, PLX4032, RG 7204, RG-7204, RO 5185426, RO-5185426, Vemurafenib, Zelboraf, VEMURAFENIB, SID137275900, Vermurafenib, vemurafenib
Patent coverage: 6,490 distinct patent families (15,704 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 15,314 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
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 |
|---|---|---|---|---|---|
| BRAF | B-Raf proto-oncogene, serine/threonine kinase | Inhibition | 8.54 | 8.6% | P15056 |
| RAF1 | Raf-1 proto-oncogene, serine/threonine kinase | Inhibition | 7.32 | P04049 |
Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Serine/threonine-protein kinase A-Raf, Receptor-interacting serine/threonine-protein kinase 3, RAF proto-oncogene serine/threonine-protein kinase, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Progesterone receptor, Muscarinic acetylcholine receptor M2, Dual specificity mitogen-activated protein kinase kinase; MEK1/2, Muscarinic acetylcholine receptor M1, GTPase KRas.
Bioactivity
ChEMBL activities: 109 potent at pChembl ≥ 5 of 119 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ARAF | 8.68 | IC50 | 2.1 | nM | CHEMBL_ACT_18231155 |
| ARAF | 8.68 | IC50 | 2.1 | nM | CHEMBL_ACT_18951182 |
| BRAF | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_13317268 |
| BRAF | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_16577211 |
| MAP3K20 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_25480615 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_26023242 |
| BRAF | 8.21 | IC50 | 6.1 | nM | CHEMBL_ACT_15605041 |
| BRAF | 8.16 | IC50 | 6.9 | nM | CHEMBL_ACT_18231167 |
| BRAF | 8.16 | IC50 | 6.9 | nM | CHEMBL_ACT_18951188 |
| P47809 | 8.09 | Kd | 8.2 | nM | CHEMBL_ACT_23172103 |
| BRAF | 8.02 | IC50 | 9.6 | nM | CHEMBL_ACT_19094008 |
| BRAF | 8 | Kd | 10 | nM | CHEMBL_ACT_25653262 |
| BRAF | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_24998822 |
| BRAF | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_25500426 |
| BRAF | 7.77 | IC50 | 17 | nM | CHEMBL_ACT_16578213 |
| TNK2 | 7.72 | IC50 | 19 | nM | CHEMBL_ACT_25112618 |
| TNK2 | 7.72 | IC50 | 19 | nM | CHEMBL_ACT_25532660 |
| BRAF | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_16577173 |
| BRAF | 7.68 | IC50 | 21 | nM | CHEMBL_ACT_13317267 |
| BRAF | 7.68 | IC50 | 21 | nM | CHEMBL_ACT_18653819 |
| BRAF | 7.68 | IC50 | 21 | nM | CHEMBL_ACT_19098102 |
| BRAF | 7.64 | IC50 | 23 | nM | CHEMBL_ACT_14975801 |
| MAP3K20 | 7.64 | IC50 | 23 | nM | CHEMBL_ACT_18255325 |
| BRAF | 7.58 | IC50 | 26 | nM | CHEMBL_ACT_14571422 |
| P28028 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_18788650 |
| BRAF | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_12114911 |
| BRAF | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_16597917 |
| BRAF | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_18528068 |
| BRAF | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_18745562 |
| BRAF | 7.51 | IC50 | 30.9 | nM | CHEMBL_ACT_18745809 |
Target pathways
Aggregated over 2 target gene(s): BRAF, RAF1.
Top Reactome pathways
44 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| RAF activation | 2 | BRAF, RAF1 |
| MAP2K and MAPK activation | 2 | BRAF, RAF1 |
| Negative feedback regulation of MAPK pathway | 2 | BRAF, RAF1 |
| Negative regulation of MAPK pathway | 2 | BRAF, RAF1 |
| Signaling by moderate kinase activity BRAF mutants | 2 | BRAF, RAF1 |
| Signaling by high-kinase activity BRAF mutants | 2 | BRAF, RAF1 |
| Signaling by BRAF and RAF1 fusions | 2 | BRAF, RAF1 |
| Paradoxical activation of RAF signaling by kinase inactive BRAF | 2 | BRAF, RAF1 |
| Signaling downstream of RAS mutants | 2 | BRAF, RAF1 |
| Signaling by RAF1 mutants | 2 | BRAF, RAF1 |
| SHOC2 M1731 mutant abolishes MRAS complex function | 2 | BRAF, RAF1 |
| Gain-of-function MRAS complexes activate RAF signaling | 2 | BRAF, RAF1 |
| Spry regulation of FGF signaling | 1 | BRAF |
| Signal Transduction | 1 | BRAF |
| Disease | 1 | BRAF |
| Signaling by NTRKs | 1 | BRAF |
| Prolonged ERK activation events | 1 | BRAF |
| Frs2-mediated activation | 1 | BRAF |
| ARMS-mediated activation | 1 | BRAF |
| Signaling by NTRK1 (TRKA) | 1 | BRAF |
| Signalling to ERKs | 1 | BRAF |
| Signalling to p38 via RIT and RIN | 1 | BRAF |
| Signaling by FGFR | 1 | BRAF |
| Stimuli-sensing channels | 1 | RAF1 |
| Rap1 signalling | 1 | RAF1 |
| GP1b-IX-V activation signalling | 1 | RAF1 |
| CD209 (DC-SIGN) signaling | 1 | RAF1 |
| Negative regulation of FGFR1 signaling | 1 | BRAF |
| Negative regulation of FGFR2 signaling | 1 | BRAF |
| Negative regulation of FGFR3 signaling | 1 | BRAF |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| MAPK cascade | 2 |
| protein phosphorylation | 2 |
| thyroid gland development | 2 |
| positive regulation of peptidyl-serine phosphorylation | 2 |
| somatic stem cell population maintenance | 2 |
| negative regulation of apoptotic process | 2 |
| thymus development | 2 |
| face development | 2 |
| signal transduction | 2 |
| cell differentiation | 2 |
| myeloid progenitor cell differentiation | 1 |
| epidermal growth factor receptor signaling pathway | 1 |
| visual learning | 1 |
| animal organ morphogenesis | 1 |
| positive regulation of gene expression | 1 |
Indications & clinical
Indications
22 indications (5 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 |
|---|---|---|---|
| melanoma | 4 | MONDO:0005105 | EFO:0000756 |
| metastatic melanoma | 4 | MONDO:0005191 | EFO:0002617 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| cutaneous melanoma | 4 | MONDO:0005012 | EFO:0000389 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| craniopharyngioma | 2 | MONDO:0018907 | EFO:1000209 |
| hairy cell leukemia | 2 | MONDO:0018935 | EFO:1000956 |
| colorectal carcinoma | 2 | MONDO:0024331 | EFO:1001951 |
| colorectal adenocarcinoma | 2 | MONDO:0005008 | EFO:0000365 |
| Langerhans cell histiocytosis | 2 | MONDO:0018310 | EFO:1000318 |
| thyroid gland carcinoma | 2 | MONDO:0015075 | EFO:0002892 |
| histiocytosis | 2 | MONDO:0002637 | HP:0100727 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| skin neoplasm | 1 | MONDO:0002531 | MONDO:0002898 |
| paraganglioma | 0 | MONDO:0000448 | EFO:1000453 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 132.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 60 |
| PHASE1 | 41 |
| PHASE3 | 9 |
| PHASE1/PHASE2 | 8 |
| Not specified | 6 |
| PHASE4 | 3 |
| EARLY_PHASE1 | 3 |
| PHASE2/PHASE3 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01683188 | PHASE4 | TERMINATED | HD IL-2 + Vemurafenib in Patients With BRAF Mutation Positive Metastatic Melanoma |
| NCT01739764 | PHASE4 | COMPLETED | An Extension (Rollover) Study of Vemurafenib in Participants With BRAF V600 Mutation-Positive Malignancies Previously Enrolled in an Antecedent Vemurafenib Protocol |
| NCT01898585 | PHASE4 | COMPLETED | An Open-Label Study of Zelboraf (Vemurafenib) in Patients With Braf V600 Mutation Positive Metastatic Melanoma |
| NCT03178552 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT03768063 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study |
| NCT05768178 | PHASE2/PHASE3 | RECRUITING | DETERMINE Trial Treatment Arm 05: Vemurafenib in Combination With Cobimetinib in Adult Patients With BRAF Positive Cancers. |
| NCT01006980 | PHASE3 | COMPLETED | A Study of Vemurafenib (RO5185426) in Comparison With Dacarbazine in Previously Untreated Patients With Metastatic Melanoma (BRIM 3) |
| NCT01307397 | PHASE3 | COMPLETED | A Study of Vemurafenib in Participants With Metastatic Melanoma |
| NCT01597908 | PHASE3 | COMPLETED | Dabrafenib Plus Trametinib vs Vemurafenib Alone in Unresectable or Metastatic BRAF V600E/K Cutaneous Melanoma |
| NCT01667419 | PHASE3 | COMPLETED | A Study of Vemurafenib Adjuvant Therapy in Participants With Surgically Resected Cutaneous BRAF-Mutant Melanoma |
| NCT01689519 | PHASE3 | COMPLETED | A Study Comparing Vemurafenib Versus Vemurafenib Plus Cobimetinib in Participants With Metastatic Melanoma |
| NCT01909453 | PHASE3 | COMPLETED | Study Comparing Combination of LGX818 Plus MEK162 Versus Vemurafenib and LGX818 Monotherapy in BRAF Mutant Melanoma |
| NCT02427893 | PHASE3 | WITHDRAWN | Trial of Vemurafenib and Cobimetinib in Patients With Advanced BRAFV600 Mutant Melanoma |
| NCT02908672 | PHASE3 | COMPLETED | A Study of Atezolizumab Plus Cobimetinib and Vemurafenib Versus Placebo Plus Cobimetinib and Vemurafenib in Previously Untreated BRAFv600 Mutation-Positive Patients With Metastatic or Unresectable Locally Advanced Melanoma |
| NCT01638676 | PHASE1/PHASE2 | RECRUITING | A Phase I/II Trial of Vemurafenib and Metformin to Melanoma Patients |
| NCT02304809 | PHASE2 | ACTIVE_NOT_RECRUITING | Phase 2 Study Assessing Secured Access to Vemurafenib for Patients With Tumors Harboring BRAF Genomic Alterations |
| NCT02693535 | PHASE2 | RECRUITING | TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT03155620 | PHASE2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) |
| NCT03181100 | PHASE2 | ACTIVE_NOT_RECRUITING | Atezolizumab With Chemotherapy in Treating Patients With Anaplastic or Poorly Differentiated Thyroid Cancer |
| NCT03224767 | PHASE2 | ACTIVE_NOT_RECRUITING | Vemurafenib and Cobimetinib in Treating Patients With BRAF V600E Mutation Positive Craniopharyngioma |
| NCT03410875 | PHASE2 | ACTIVE_NOT_RECRUITING | A Phase II Study of the BRAF Inhibitor, Vemurafenib, Plus Obinutuzumab in Patients With Previously Untreated Classical Hairy Cell Leukemia |
| NCT04302025 | PHASE2 | RECRUITING | A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) |
| NCT04423185 | PHASE2 | RECRUITING | PLATFORM Study of Precision Medicine for Rare Tumors |
| NCT04943198 | PHASE2 | RECRUITING | Optimization of the Time and Dosage of Vemurafenib in BRAF Positive Juvenile Patients With Refractory Histiocytosis |
| NCT05159245 | PHASE2 | RECRUITING | The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs |
| NCT06440850 | PHASE2 | RECRUITING | Vemurafenib and Cobimetinib for the Treatment of Patients With High Risk Differentiated Thyroid Carcinoma With BRAFV600E Mutation |
| NCT06561360 | PHASE2 | RECRUITING | A Study of Vemurafenib and Obinutuzumab Compared to Cladribine and Rituximab in People With Hairy Cell Leukemia (HCL) |
| NCT06603376 | PHASE2 | RECRUITING | Irinotecan Hydrochloride Liposome Injection (Ⅱ) Combined with Fluorouracil, Folinic Acid, Vermofenib and Cetuximab in First-line Treatment of BRAFV600E Mutated Advanced Colorectal Cancer |
| NCT06692491 | PHASE2 | NOT_YET_RECRUITING | Study of Precision Treatment for Rare Tumours in China Guided by PDO and NGS |
| NCT00949702 | PHASE2 | COMPLETED | A Study of Vemurafenib in Previously Treated Patients With Metastatic Melanoma |
| NCT01286753 | PHASE2 | COMPLETED | A Study of Vemurafenib (RO5185426) in Participants With Metastatic or Unresectable Papillary Thyroid Cancer Positive for the BRAF V600 Mutation |
| NCT01378975 | PHASE2 | COMPLETED | A Study of Vemurafenib in Metastatic Melanoma Participants With Brain Metastases |
| NCT01474551 | PHASE2 | TERMINATED | Vemurafenib (R05185426) in Poor Performance Status Patients With Unresectable Locally Advanced or Metastatic Melanoma Harboring a V600E/K Mutation |
| NCT01495988 | PHASE2 | TERMINATED | Trial of Vemurafenib/Cobimetinib With or Without Bevacizumab in Patients With Stage IV BRAFV600 Mutant Melanoma |
| NCT01524978 | PHASE2 | COMPLETED | A Study of Vemurafenib in Participants With BRAF V600 Mutation-Positive Cancers |
| NCT01586195 | PHASE2 | TERMINATED | Study Of Zelboraf (Vemurafenib) in Patients With Locally-Advanced, Unresectable, Stage IIIc Or Metastatic Melanoma and Activating Exon 15 BRAF Mutations Other Than V600E |
| NCT01616199 | PHASE1/PHASE2 | TERMINATED | Study of PX-866 and Vemurafenib in Patients With Advanced Melanoma |
| NCT01659151 | PHASE2 | COMPLETED | Vemurafenib With Lymphodepletion Plus Adoptive Cell Transfer & High Dose IL-2 Metastatic Melanoma |
| NCT01673854 | PHASE2 | COMPLETED | Phase II Safety Study of Vemurafenib Followed by Ipilimumab in Subjects With V600 BRAF Mutated Advanced Melanoma |
Clinical evidence (CIViC)
Variant × indication × effect (186 predictive associations from 251 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| BRAF V600 | Melanoma | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC A | EID6044 +1 |
| BRAF V600E | Skin Melanoma | Sensitivity/Response | Vemurafenib | CIViC A | EID1409 +1 |
| BRAF V600 | Erdheim-Chester Disease | Sensitivity/Response | Vemurafenib | CIViC A | EID11237 |
| BRAF V600 | Melanoma | Sensitivity/Response | Atezolizumab + Vemurafenib + Cobimetinib | CIViC A | EID11238 |
| BRAF V600E | Melanoma | Sensitivity/Response | Vemurafenib | CIViC B | EID1398 +14 |
| BRAF V600K | Melanoma | Sensitivity/Response | Vemurafenib | CIViC B | EID1399 +9 |
| BRAF V600E | Hairy Cell Leukemia | Sensitivity/Response | Vemurafenib | CIViC B | EID11315 +6 |
| BRAF V600E | Colorectal Cancer | Sensitivity/Response | Vemurafenib | CIViC B | EID1405 +4 |
| BRAF V600E | Papillary Thyroid Carcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID1591 +4 |
| BRAF V600E | Lung Adenocarcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID3782 +3 |
| BRAF V600 | Langerhans-cell Histiocytosis | Sensitivity/Response | Vemurafenib | CIViC B | EID11302 +1 |
| BRAF V600E | Colorectal Cancer | Sensitivity/Response | Panitumumab + Vemurafenib | CIViC B | EID1413 +1 |
| BRAF V600E | Colorectal Cancer | Sensitivity/Response | Vemurafenib + Irinotecan + Cetuximab | CIViC B | EID1902 +1 |
| BRAF V600E | Anaplastic Thyroid Carcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID6045 +1 |
| BRAF V600E | Lung Non-small Cell Carcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID5958 +1 |
| BRAF K601E | Cancer | Sensitivity/Response | Vemurafenib | CIViC B | EID5963 |
| BRAF V600 | Melanoma | Sensitivity/Response | Vemurafenib + Cobimetinib | CIViC B | EID1422 |
| BRAF V600 | Lung Non-small Cell Carcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID1574 |
| BRAF V600 | Colorectal Cancer | Sensitivity/Response | Vemurafenib + Cetuximab | CIViC B | EID1598 |
| BRAF V600 | Cholangiocarcinoma | Sensitivity/Response | Vemurafenib | CIViC B | EID5905 |
| BRAF V600 | Colorectal Cancer | Sensitivity/Response | Cetuximab + Vemurafenib + Irinotecan | CIViC B | EID7355 |
| BRAF V600E | Colorectal Cancer | Sensitivity/Response | Erlotinib + Vemurafenib | CIViC B | EID11427 |
| BRAF V600E | Low Grade Glioma | Sensitivity/Response | Vemurafenib | CIViC B | EID11770 |
| BRAF V600E | Melanoma | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC B | EID1421 |
| BRAF V600E | Ovarian Cancer | Sensitivity/Response | Vemurafenib | CIViC B | EID5959 |
| BRAF V600E | Langerhans Cell Sarcoma | Sensitivity/Response | Vemurafenib | CIViC B | EID7583 |
| BRAF V600E OR BRAF K601E | Colorectal Cancer | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC B | EID11670 |
| BRAF L505H | Melanoma | Resistance | Vemurafenib | CIViC B | EID1669 +1 |
| MET Overexpression | Skin Melanoma | Resistance | Vemurafenib | CIViC B | EID1581 +1 |
| RAC1 P29S | Melanoma | Resistance | Vemurafenib + Dabrafenib | CIViC B | EID7669 +1 |
+156 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
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.
51 molecules share ≥1 primary target. Top 51 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, RAF1 |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, RAF1 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, RAF1 |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| DASATINIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| IMATINIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| NILOTINIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| TOVORAFENIB | ChEMBL | Phase 4 (approved) | BRAF, RAF1 |
| AVUTOMETINIB | ChEMBL | Phase 3 | BRAF, RAF1 |
| MOTESANIB | ChEMBL | Phase 3 | BRAF, RAF1 |
| NAPORAFENIB | ChEMBL | Phase 3 | BRAF, RAF1 |
| BELVARAFENIB | ChEMBL | Phase 2 | BRAF, RAF1 |
| BRIMARAFENIB | ChEMBL | Phase 2 | BRAF, RAF1 |
| CEP-32496 | ChEMBL | Phase 2 | BRAF, RAF1 |
| DORAMAPIMOD | ChEMBL | Phase 2 | BRAF, RAF1 |
| EXARAFENIB | ChEMBL | Phase 2 | BRAF, RAF1 |
| FORETINIB | ChEMBL | Phase 2 | BRAF, RAF1 |
| R-406 | ChEMBL | Phase 2 | BRAF, RAF1 |
| RAF-265 | ChEMBL | Phase 2 | BRAF, RAF1 |
| REBASTINIB | ChEMBL | Phase 2 | BRAF, RAF1 |
| Afatinib | PubChem | Approved | BRAF, RAF1 |
| Crizotinib | PubChem | Approved | BRAF, RAF1 |
| Idelalisib | PubChem | Approved | BRAF, RAF1 |
| Selumetinib | PubChem | Approved | BRAF, RAF1 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | BRAF |
| COBIMETINIB | ChEMBL | Phase 4 (approved) | BRAF |
| ENCORAFENIB | ChEMBL | Phase 4 (approved) | BRAF |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | BRAF |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | BRAF |
| PONATINIB | ChEMBL | Phase 4 (approved) | BRAF |
| RUXOLITINIB | ChEMBL | Phase 4 (approved) | BRAF |
| MASITINIB | ChEMBL | Phase 3 | BRAF |
| PLINABULIN | ChEMBL | Phase 3 | RAF1 |
| QUERCETIN | ChEMBL | Phase 3 | BRAF |
| BAFETINIB | ChEMBL | Phase 2 | BRAF |
| CI-1040 | ChEMBL | Phase 2 | RAF1 |
| ELLAGIC ACID | ChEMBL | Phase 2 | BRAF |
| LIFIRAFENIB | ChEMBL | Phase 2 | BRAF |
| MIRDAMETINIB | ChEMBL | Phase 2 | BRAF |
| PEXMETINIB | ChEMBL | Phase 2 | BRAF |
| RISOVALISIB | ChEMBL | Phase 2 | RAF1 |
| TG100-115 | ChEMBL | Phase 2 | BRAF |
| TINLORAFENIB | ChEMBL | Phase 2 | BRAF |
| TOLONIUM CHLORIDE | ChEMBL | Phase 2 | RAF1 |
| XL-281 | ChEMBL | Phase 2 | BRAF |
| Binimetinib | PubChem | Approved | BRAF |
| dacomitinib | PubChem | Approved | BRAF |
| Fostamatinib | PubChem | Approved | BRAF |
| Trametinib | PubChem | Approved | BRAF |
Related Atlas pages
- Genes: BRAF, RAF1
- Diseases: melanoma, metastatic melanoma, neoplasm, cutaneous melanoma, Erdheim-Chester disease, hairy cell leukemia, colorectal carcinoma, thyroid gland papillary carcinoma, lung adenocarcinoma, Langerhans cell histiocytosis specific to childhood, thyroid gland undifferentiated (anaplastic) carcinoma, cancer, cholangiocarcinoma, low grade glioma, ovarian carcinoma, Langerhans cell sarcoma
- Drugs: Gefitinib, Pazopanib, Regorafenib, Dabrafenib, Dasatinib, Erlotinib, Imatinib, Nilotinib, Sorafenib, Tovorafenib, Avutometinib, Motesanib, Naporafenib, Afatinib, Crizotinib, Idelalisib, Selumetinib, Abemaciclib, Cobimetinib, Encorafenib, Fedratinib, Infigratinib, Ponatinib, Ruxolitinib, Masitinib, Plinabulin, Quercetin, Binimetinib, dacomitinib, Fostamatinib, Trametinib
- Biomarker genes: AKT1, AKT3, GNAQ, HRAS, MAP2K1, NF1, NRAS, PIK3R2, PREX2, RNASE3, SLTM, SOX10, STAG2, STAG3