Dabrafenib

Summary

Dabrafenib (CHEMBL2028663) is an approved small-molecule antineoplastic agent (ATC L01EC02) that acts as a serine/threonine-protein kinase B-raf inhibitor, targeting BRAF; approved for 7 indications including neoplasm and melanoma, and in clinical trials for 7 other conditions; with CIViC clinical evidence for 80 variant-indication associations (e.g. BRAF V600E in melanoma).

At a glance

• Status: FDA-approved (also EMA, PMDA)
• Modality: Small molecule
• ATC class: L01EC02
• Targets: 1 (BRAF) (top 2% of drugs corpus-wide)
• Indications: 22 conditions (top 10% of drugs corpus-wide)
• Clinical trials: 138
• Precision-oncology evidence (CIViC): 80 variant–indication associations
• Chemistry: 519.6 Da · C23H20F3N5O2S2
• Target biology: 1 curated target implicated as cohort gene in 102 diseases corpus-wide; indicated or in trials for 18 (8 on both)
• Competitive landscape: target BRAF is also targeted by 6 other curated drugs in the corpus

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2028663
Name	Dabrafenib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	44462760
ChEBI	CHEBI:75045
ATC	L01EC02
Molecular formula	C23H20F3N5O2S2
Molecular weight	519.6
InChIKey	BFSMGDJOXZAERB-UHFFFAOYSA-N

SMILES: CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

IUPAC name: N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide

ChEBI definition: An organofluorine compound and antineoplastic agent, used as its mesylate salt in treatment of metastatic melanoma.

Pharmacological roles (ChEBI): antineoplastic agent, B-Raf inhibitor, anticoronaviral agent.

Also known as: Dabrafenib, GSK-2118436, GSK-2118436A, Gsk2118436, GSK2118436A, Tafinlar, DABRAFENIB, SID174006404, dabrafenib, Dabrafenib; Tafinlar, DABRAFENIB (GSK2118436), Dabrafenib (GSK2118436)

Parent form; salt/anhydrous children: CHEMBL2105729

Patent coverage: 5,200 distinct patent families (13,060 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 12,339 (94%) 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	8.49	8.6%	P15056

Mechanism of action (ChEMBL curated)

Target gene: BRAF

Mechanism of action	Action type	Target	Target type
Serine/threonine-protein kinase B-raf inhibitor	INHIBITOR	Serine/threonine-protein kinase B-raf	SINGLE PROTEIN

Broader ChEMBL bioactivity targets: 55 (assay-derived screening hits — not curated targets; per-target potencies are in the ChEMBL bioactivities table below).

Bioactivity

ChEMBL activities: 91 potent at pChembl ≥ 5 of 93 total. Top 80 distinct by potency (10 = 0.1 nM, 6 = 1 µM):

Protein	UniProt	Gene	pChembl	Type	Value	Activity ID
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.4	IC50	0.4 nM	CHEMBL_ACT_16577174
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.3	IC50	0.5 nM	CHEMBL_ACT_22885302
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.22	IC50	0.6 nM	CHEMBL_ACT_25708394
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.19	IC50	0.65 nM	CHEMBL_ACT_26027115
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.15	IC50	0.7 nM	CHEMBL_ACT_12691522
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.15	IC50	0.71 nM	CHEMBL_ACT_18745826
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.15	EC50	0.7 nM	CHEMBL_ACT_24882829
Serine/threonine-protein kinase B-raf	P15056	BRAF	9.1	IC50	0.8 nM	CHEMBL_ACT_18528065
Serine/threonine-protein kinase B-raf	P15056	BRAF	9	IC50	1 nM	CHEMBL_ACT_16577212
Receptor-interacting serine/threonine-protein kinase 3	Q9Y572	RIPK3	8.7	IC50	2 nM	CHEMBL_ACT_19146734
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.7	IC50	2 nM	CHEMBL_ACT_26023197
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.49	IC50	3.2 nM	CHEMBL_ACT_26023196
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.4	IC50	4 nM	CHEMBL_ACT_12691436
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.3	IC50	5 nM	CHEMBL_ACT_18946042
RAF proto-oncogene serine/threonine-protein kinase	P04049	RAF1	8.3	IC50	5 nM	CHEMBL_ACT_25708393
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.22	IC50	6 nM	CHEMBL_ACT_15605136
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.1	IC50	8 nM	CHEMBL_ACT_12691441
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.05	IC50	9 nM	CHEMBL_ACT_16673781
Serine/threonine-protein kinase B-raf	P15056	BRAF	8.01	IC50	9.7 nM	CHEMBL_ACT_15605028
Serine/threonine-protein kinase B-raf	P15056	BRAF	7.96	IC50	11 nM	CHEMBL_ACT_15605005
Cyclin-dependent kinase 16	Q00536	CDK16	7.89	Kd	13 nM	CHEMBL_ACT_17889418
Cyclin-dependent kinase 2	P24941	CDK2	7.72	Kd	19 nM	CHEMBL_ACT_17889735
Serine/threonine-protein kinase B-raf	P15056	BRAF	7.66	Kd	22 nM	CHEMBL_ACT_17885918
Serine/threonine-protein kinase A-Raf	P10398	ARAF	7.58	IC50	26 nM	CHEMBL_ACT_15605133
LIM domain kinase 1	P53667	LIMK1	7.48	Kd	33 nM	CHEMBL_ACT_17909720
Serine/threonine-protein kinase D2	Q9BZL6	PRKD2	7.47	Kd	34 nM	CHEMBL_ACT_17931324
Cyclin-dependent kinase 17	Q00537	CDK17	7.44	Kd	36 nM	CHEMBL_ACT_17889510
Serine/threonine-protein kinase A-Raf	P10398	ARAF	7.33	Kd	47 nM	CHEMBL_ACT_17883691
Serine/threonine-protein kinase Nek9	Q8TD19	NEK9	7.28	Kd	53 nM	CHEMBL_ACT_17921847
Non-receptor tyrosine-protein kinase TNK1	Q13470	TNK1	7.18	Kd	66 nM	CHEMBL_ACT_17945500
Receptor-interacting serine/threonine-protein kinase 2	O43353	RIPK2	7.11	IC50	77 nM	CHEMBL_ACT_19146735
LIM domain kinase 2	P53671	LIMK2	7.09	Kd	82 nM	CHEMBL_ACT_17909990
Nuclear receptor subfamily 1 group I member 2	O75469	NR1I2	7.09	EC50	82 nM	CHEMBL_ACT_26023198
Nuclear receptor subfamily 1 group I member 2	O75469	NR1I2	7.06	EC50	87.2 nM	CHEMBL_ACT_24882851
Nuclear receptor subfamily 1 group I member 2	O75469	NR1I2	7.06	EC50	87 nM	CHEMBL_ACT_24882865
Receptor-interacting serine/threonine-protein kinase 2	O43353	RIPK2	6.97	Kd	106 nM	CHEMBL_ACT_17935367
Serine/threonine-protein kinase/endoribonuclease IRE2	Q76MJ5	ERN2	6.94	Kd	116 nM	CHEMBL_ACT_17901986
Serine/threonine-protein kinase D3	O94806	PRKD3	6.92	Kd	120 nM	CHEMBL_ACT_17931475
Cyclin-dependent kinase 4	P11802	CDK4	6.9	Kd	126 nM	CHEMBL_ACT_17890418
RAF proto-oncogene serine/threonine-protein kinase	P04049	RAF1	6.82	IC50	150 nM	CHEMBL_ACT_15605139
Mitogen-activated protein kinase kinase kinase 20	Q9NYL2	MAP3K20	6.74	Kd	184 nM	CHEMBL_ACT_17948549
Serine/threonine-protein kinase ULK1	O75385	ULK1	6.73	Kd	188 nM	CHEMBL_ACT_17947234
Receptor-interacting serine/threonine-protein kinase 3	Q9Y572	RIPK3	6.6	IC50	250 nM	CHEMBL_ACT_19146732
Receptor-interacting serine/threonine-protein kinase 3	Q9Y572	RIPK3	6.55	Kd	283 nM	CHEMBL_ACT_17935512
Tyrosine-protein kinase ABL2	P42684	ABL2	6.52	Kd	305 nM	CHEMBL_ACT_17878652
Cyclin-dependent kinase 6	Q00534	CDK6	6.5	Kd	318 nM	CHEMBL_ACT_17890906
Cyclin-dependent kinase 1	P06493	CDK1	6.44	Kd	364 nM	CHEMBL_ACT_17888561
Ephrin type-B receptor 6	O15197	EPHB6	6.38	Kd	412 nM	CHEMBL_ACT_17901223
Serine/threonine-protein kinase Nek1	Q96PY6	NEK1	6.32	Kd	477 nM	CHEMBL_ACT_17921052
Serine/threonine-protein kinase B-raf	P15056	BRAF	6.28	EC50	529 nM	CHEMBL_ACT_16578179
Serine/threonine-protein kinase PLK4	O00444	PLK4	6.28	Kd	520 nM	CHEMBL_ACT_17928004
Activin receptor type-1B	P36896	ACVR1B	6.22	Kd	601 nM	CHEMBL_ACT_17880867
Serine/threonine-protein kinase SIK2	Q9H0K1	SIK2	6.19	Kd	649 nM	CHEMBL_ACT_17938082
Ephrin type-A receptor 1	P21709	EPHA1	6.15	Kd	705 nM	CHEMBL_ACT_17899187
Tyrosine-protein kinase FRK	P42685	FRK	6.14	Kd	727 nM	CHEMBL_ACT_17903956
Tyrosine-protein kinase Lck	P06239	LCK	6.11	Kd	783 nM	CHEMBL_ACT_17909435
Tyrosine-protein kinase Fyn	P06241	FYN	6.09	Kd	817 nM	CHEMBL_ACT_17904176
Tyrosine-protein kinase CSK	P41240	CSK	6.07	Kd	851 nM	CHEMBL_ACT_17893310
Eukaryotic translation initiation factor 2-alpha kinase 1	Q9BQI3	EIF2AK1	6.02	Kd	949 nM	CHEMBL_ACT_17898731
Mitogen-activated protein kinase kinase kinase 11	Q16584	MAP3K11	6	Kd	1011 nM	CHEMBL_ACT_17911988
Cyclin-dependent kinase 5	Q00535	CDK5	5.97	Kd	1068 nM	CHEMBL_ACT_17890645
Tyrosine-protein kinase Yes	P07947	YES1	5.89	Kd	1276 nM	CHEMBL_ACT_17948241
Tyrosine-protein kinase Lyn	P07948	LYN	5.87	Kd	1353 nM	CHEMBL_ACT_17910254
Protein-tyrosine kinase 6	Q13882	PTK6	5.85	Kd	1414 nM	CHEMBL_ACT_17932959
Serine/threonine-protein kinase/endoribonuclease IRE1	O75460	ERN1	5.84	Kd	1453 nM	CHEMBL_ACT_17901681
Serine/threonine-protein kinase ULK3	Q6PHR2	ULK3	5.83	Kd	1480 nM	CHEMBL_ACT_17947497
Tyrosine-protein kinase ABL1	P00519	ABL1	5.81	Kd	1545 nM	CHEMBL_ACT_17878489
Tyrosine-protein kinase Fgr	P09769	FGR	5.81	Kd	1549 nM	CHEMBL_ACT_17903408
Interleukin-1 receptor-associated kinase 1	P51617	IRAK1	5.81	Kd	1564 nM	CHEMBL_ACT_17908048
Hepatocyte growth factor receptor	P08581	MET	5.79	Kd	1634 nM	CHEMBL_ACT_17918995
Tyrosine-protein kinase HCK	P08631	HCK	5.78	Kd	1646 nM	CHEMBL_ACT_17905990
Maternal embryonic leucine zipper kinase	Q14680	MELK	5.74	Kd	1816 nM	CHEMBL_ACT_17918655
Serine/threonine-protein kinase SIK3	Q9Y2K2	SIK3	5.7	Kd	2005 nM	CHEMBL_ACT_17938311
Calcium/calmodulin-dependent protein kinase type IV	Q16566	CAMK4	5.64	Kd	2274 nM	CHEMBL_ACT_17887103
Dual specificity mitogen-activated protein kinase kinase 5	Q13163	MAP2K5	5.64	Kd	2294 nM	CHEMBL_ACT_17911323
TGF-beta receptor type-1	P36897	TGFBR1	5.62	Kd	2384 nM	CHEMBL_ACT_17944648
TGF-beta receptor type-2	P37173	TGFBR2	5.6	Kd	2534 nM	CHEMBL_ACT_17944879
Tyrosine-protein kinase JAK2	O60674	JAK2	5.49	Kd	3223 nM	CHEMBL_ACT_17909037
TGF-beta receptor type-1	P36897	TGFBR1	5.43	IC50	3700 nM	CHEMBL_ACT_12691437
GTPase KRas	P01116	KRAS	5.23	IC50	5880 nM	CHEMBL_ACT_15604993

Target pathways

Aggregated over 1 target gene(s): BRAF.

Top Reactome pathways

39 total, by targets touching each:

Pathway	Targets	Genes
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
Negative regulation of FGFR1 signaling	1	BRAF
Negative regulation of FGFR2 signaling	1	BRAF
Negative regulation of FGFR3 signaling	1	BRAF
Negative regulation of FGFR4 signaling	1	BRAF
Signaling by FGFR1	1	BRAF
Signaling by FGFR2	1	BRAF
Signaling by FGFR3	1	BRAF
Signaling by FGFR4	1	BRAF
Diseases of signal transduction by growth factor receptors and second messengers	1	BRAF
RAF activation	1	BRAF
RAF/MAP kinase cascade	1	BRAF
MAP2K and MAPK activation	1	BRAF
Negative feedback regulation of MAPK pathway	1	BRAF
Negative regulation of MAPK pathway	1	BRAF
MAPK family signaling cascades	1	BRAF
MAPK1/MAPK3 signaling	1	BRAF
Signaling by moderate kinase activity BRAF mutants	1	BRAF
Signaling by high-kinase activity BRAF mutants	1	BRAF
Signaling by RAS mutants	1	BRAF
Signaling by BRAF and RAF1 fusions	1	BRAF
Paradoxical activation of RAF signaling by kinase inactive BRAF	1	BRAF
Oncogenic MAPK signaling	1	BRAF
Signaling by Receptor Tyrosine Kinases	1	BRAF
Signaling downstream of RAS mutants	1	BRAF
Signaling by RAF1 mutants	1	BRAF
Signaling by MRAS-complex mutants	1	BRAF
SHOC2 M1731 mutant abolishes MRAS complex function	1	BRAF
Gain-of-function MRAS complexes activate RAF signaling	1	BRAF

Dominant GO biological processes

GO term	Targets
MAPK cascade	1
protein phosphorylation	1
epidermal growth factor receptor signaling pathway	1
animal organ morphogenesis	1
positive regulation of gene expression	1
positive regulation of D-glucose transmembrane transport	1
positive regulation of peptidyl-serine phosphorylation	1
negative regulation of apoptotic process	1
positive regulation of ERK1 and ERK2 cascade	1
cellular response to calcium ion	1
establishment of protein localization to membrane	1
postsynaptic modulation of chemical synaptic transmission	1
signal transduction	1

Predicted targets — Sugi Predict

This molecule is SureChEMBL compound SCHEMBL29350038 — see its predicted protein targets + similar patent compounds on Sugi Predict.

Indications & clinical

Indications

7 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
melanoma	3	MONDO:0005105	EFO:0000756
cutaneous melanoma	3	MONDO:0005012	EFO:0000389
thyroid gland papillary carcinoma	3	MONDO:0005075	EFO:0000641
metastatic melanoma	3	MONDO:0005191	EFO:0002617
thyroid gland carcinoma	3	MONDO:0015075	EFO:0002892
ameloblastoma	3	MONDO:0017795

7 diseases in clinical trials (phase 2–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
thyroid gland follicular carcinoma	2	MONDO:0005034	EFO:0000501
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
Erdheim-Chester disease	2	MONDO:0018153	EFO:1000926
lung neoplasm	2	MONDO:0021117
undifferentiated carcinoma	2	MONDO:0005617	EFO:0006772
craniopharyngioma	2	MONDO:0018907	EFO:1000209
thyroid gland undifferentiated (anaplastic) carcinoma	2	MONDO:0006468	EFO:1000595

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

Regulatory approval & mechanism (DrugCentral)

Approved: FDA, EMA, PMDA. Curated mechanism: INHIBITOR · 1 MOA target of 9 total (P15056).

DrugCentral (CC BY-SA): authoritative regulatory-approval status + curated mechanism. The drug’s full target set is in Targets above.

Clinical trials

Total trials: 138.

Phase distribution

Phase	Trials
Phase 2	60
Phase 1	31
Not specified	19
Phase 1/2	13
Phase 3	10
Phase 4	3
Phase 2/3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03340506	Phase 4	RECRUITING	Dabrafenib and/or Trametinib Rollover Study
NCT03975829	Phase 4	ACTIVE_NOT_RECRUITING	Pediatric Long-Term Follow-up and Rollover Study
NCT07010393	Phase 4	NOT_YET_RECRUITING	Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study
NCT04940052	Phase 3	ACTIVE_NOT_RECRUITING	Study of Efficacy and Safety of Dabrafenib in Combination With Trametinib in Previously Treated Patients With Metastatic, Radio-active Iodine Refractory BRAF V600E Mutation Positive Differentiated Thyroid Cancer
NCT06475989	Phase 3	RECRUITING	Study of Targeted Therapy vs. Chemotherapy in Patients With Thyroid Cancer
NCT06819605	Phase 2/3	NOT_YET_RECRUITING	Neoadjuvant Therapy With Conservative Surgery vs. Up-front Conservative Surgery for BRAF V600E-Mutated Ameloblastoma
NCT07440290	Phase 2/3	RECRUITING	DETERMINE Trial Treatment Arm 07: Dabrafenib in Combination With Trametinib in Adult, Paediatric and Teenage/Young Adult Patients With BRAF V600 Mutation-Positive Cancers.
NCT01227889	Phase 3	COMPLETED	A Study Comparing GSK2118436 to Dacarbazine (DTIC) in Previously Untreated Subjects With BRAF Mutation Positive Advanced (Stage III) or Metastatic (Stage IV) Melanoma
NCT01584648	Phase 3	COMPLETED	A Study Comparing Trametinib and Dabrafenib Combination Therapy to Dabrafenib Monotherapy in Subjects With BRAF-mutant Melanoma
NCT01597908	Phase 3	COMPLETED	Dabrafenib Plus Trametinib vs Vemurafenib Alone in Unresectable or Metastatic BRAF V600E/K Cutaneous Melanoma
NCT01682083	Phase 3	COMPLETED	Dabrafenib With Trametinib in the Adjuvant Treatment of High-risk BRAF V600 Mutation-positive Melanoma (COMBI-AD).
NCT02967692	Phase 3	TERMINATED	A Study of the Anti-PD1 Antibody PDR001, in Combination With Dabrafenib and Trametinib in Advanced Melanoma
NCT03551626	Phase 3	COMPLETED	Study of Dabrafenib+Trametinib in the Adjuvant Treatment of Stage III BRAF V600+ Melanoma After Complete Resection to Evaluate the Impact on Pyrexia Related Outcomes
NCT03784014	Phase 3	COMPLETED	Molecular Profiling of Advanced Soft-tissue Sarcomas
NCT06264778	Phase 3	UNKNOWN	Exploration of Fenestration Decompression Combined With Dalafenib in the Treatment of BRAF Mutant Ameloblastoma
NCT01989585	Phase 1/2	ACTIVE_NOT_RECRUITING	Testing the Addition of Navitoclax to the Combination of Dabrafenib and Trametinib in People Who Have BRAF Mutant Melanoma
NCT02231775	Phase 2	ACTIVE_NOT_RECRUITING	Dabrafenib and Trametinib Before and After Surgery in Treating Patients With Stage IIIB-C Melanoma With BRAF V600 Mutation
NCT02465060	Phase 2	ACTIVE_NOT_RECRUITING	Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02858921	Phase 2	ACTIVE_NOT_RECRUITING	Neoadjuvant Dabrafenib, Trametinib and/or Pembrolizumab in BRAF Mutant Resectable Stage III Melanoma
NCT02910700	Phase 2	ACTIVE_NOT_RECRUITING	Nivolumab With Trametinib and Dabrafenib, or Encorafenib and Binimetinib in Treating Patients With BRAF Mutated Metastatic or Unresectable Stage III-IV Melanoma
NCT02925234	Phase 2	RECRUITING	The Drug Rediscovery Protocol (DRUP Trial)
NCT03149029	Phase 2	ACTIVE_NOT_RECRUITING	Abbreviated MAPK Targeted Therapy Plus Pembrolizumab in Melanoma
NCT03563729	Phase 2	RECRUITING	Melanoma Metastasized to the Brain and Steroids
NCT04116541	Phase 2	RECRUITING	A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors.
NCT04201457	Phase 1/2	ACTIVE_NOT_RECRUITING	A Trial of Dabrafenib, Trametinib and Hydroxychloroquine for Patients With Recurrent LGG or HGG With a BRAF Aberration
NCT04238624	Phase 2	ACTIVE_NOT_RECRUITING	Study of Cemiplimab Combined With Dabrafenib and Trametinib in People With Anaplastic Thyroid Cancer
NCT04544111	Phase 2	ACTIVE_NOT_RECRUITING	PDR001 Combination Therapy for Radioiodine-Refractory Thyroid Cancer
NCT04675710	Phase 2	ACTIVE_NOT_RECRUITING	Pembrolizumab, Dabrafenib, and Trametinib Before Surgery for the Treatment of BRAF-Mutated Anaplastic Thyroid Cancer
NCT05159245	Phase 2	RECRUITING	The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs
NCT05525273	Phase 2	RECRUITING	Treatment of BRAF ( B-Rapidly Accelerated Fibrosarcoma) Mutated Papillary Craniopharyngioma
NCT06054191	Phase 2	NOT_YET_RECRUITING	Neoadjuvant and Adjuvant Targeted Treatment in NSCLC With BRAF V600 or MET Exon 14 Mutations
NCT06079333	Phase 2	RECRUITING	NEO- and Adjuvant Targeted Therapy in Braf-mutated Anaplastic Cancer of the Thyroid (NEO-ATACT Study)
NCT06119789	Phase 2	RECRUITING	Precision Cancer Therapy in Rare Cancers
NCT06482086	Phase 2	RECRUITING	Efficacy of Organoid-Based Drug Screening to Guide Treatment for Locally Advanced Thyroid Cancer
NCT06563999	Phase 2	RECRUITING	Neoadjuvant Umbrella Trial for Patients With Unresectable Stage III NSCLC Harboring Rare Mutations.
NCT06653517	Phase 2	RECRUITING	Clinical Study of Neoadjuvant Targeted Therapy for Ameloblastoma
NCT06712875	Phase 1/2	RECRUITING	MAPK Inhibition Combined With Anti-PD1 Therapy for BRAF-altered Pediatric Gliomas
NCT06739395	Phase 2	RECRUITING	Precision Medicine Trial Based on Molecular Matching Therapy for Patients With Standard Treatment Exhaustion
NCT07110246	Phase 2	RECRUITING	Dabrafenib and Trametinib for BRAF V600 Mutant Low-Grade Gliomas
NCT07506109	Phase 2	RECRUITING	A Phase II Study of Sintilimab Combined With Ipilimumab N01, Cetuximab and Dabrafenib in Patients With Microsatellite-Stable, BRAF V600E-Mutated Metastatic Colorectal Cancer
NCT01072175	Phase 2	COMPLETED	Investigate Safety, Pharmacokinetics and Pharmacodynamics of GSK2118436 & GSK1120212
NCT01153763	Phase 2	COMPLETED	A Study of GSK2118436 in BRAF Mutant Metastatic Melanoma
NCT01266967	Phase 2	COMPLETED	A Study of GSK2118436 in BRAF Mutant Metastatic Melanoma to the Brain
NCT01336634	Phase 2	COMPLETED	Study of Selective BRAF Kinase Inhibitor Dabrafenib Monotherapy Twice Daily and in Combination With Dabrafenib Twice Daily and Trametinib Once Daily in Combination Therapy in Subjects With BRAF V600E Mutation Positive Metastatic (Stage IV) Non-small Cell Lung Cancer.
NCT01619774	Phase 2	COMPLETED	An Open-Label Phase II Study of the Combination of GSK2118436 and GSK1120212 in Patients With Metastatic Melanoma Which is Refractory or Resistant to BRAF Inhibitor
NCT01677741	Phase 1/2	COMPLETED	A Study to Determine Safety, Tolerability and Pharmacokinetics of Oral Dabrafenib In Children and Adolescent Subjects
NCT01682213	Phase 2	COMPLETED	Adjuvant Dabrafenib (GSK2118436) in Patients With Surgically Resected AJCC Stage IIIC Melanoma Characterized by a BRAFV600E/K Mutation
NCT01701037	Phase 2	TERMINATED	Dabrafenib Alone and in Combination With Trametinib Before Surgery in Treating Patients With Locally or Regionally Advanced Melanoma That Can Be Removed By Surgery
NCT01721603	Phase 2	TERMINATED	Dabrafenib and Trametinib With Radiosurgery in Melanoma Brain Mets
NCT01723202	Phase 2	COMPLETED	Dabrafenib With or Without Trametinib in Treating Patients With Advanced Differentiated Thyroid Cancer
NCT01750918	Phase 1/2	COMPLETED	BRAF/MEK/EGFR Inhibitor Combination Study in Colorectal Cancer (CRC)
NCT01928940	Phase 2	COMPLETED	Japan PhI/II of GSK2118436 and GSK1120212 Combination in Subjects With BRAF V600E/K Mutation Positive Advanced Solid Tumors (Phase I Part) or Cutaneous Melanoma (Phase II Part)
NCT01972347	Phase 2	COMPLETED	Neoadjuvant Dabrafenib + Trametinib for AJCC Stage IIIB-C BRAF V600 Mutation Positive Melanoma
NCT01978236	Phase 2	TERMINATED	Dabrafenib/Trametinib, BRAF or BRAF AND MEK Pre-op With BRAF and MEK Post-op, Phase IIB, Melanoma With Brain Mets,Biomarkers and Metabolites
NCT02034110	Phase 2	COMPLETED	Efficacy and Safety of the Combination Therapy of Dabrafenib and Trametinib in Subjects With BRAF V600E- Mutated Rare Cancers
NCT02039947	Phase 2	COMPLETED	Study to Evaluate Treatment of Dabrafenib Plus Trametinib in Subjects With BRAF Mutation-Positive Melanoma That Has Metastasized to the Brain
NCT02052193	Phase 2	TERMINATED	Evaluation of Photosensitivity in Dabrafenib or Vemurafenib Treated Metastatic Melanoma Patients - a Phase IIa/IIb Study
NCT02083354	Phase 2	COMPLETED	Study to Investigate the Objective Response Rate of Dabrafenib in Combination With Trametinib in Subjects With BRAF V600 Mutation-Positive Melanoma
NCT02124772	Phase 1/2	COMPLETED	Study to Investigate Safety, Pharmacokinetic (PK), Pharmacodynamic (PD) and Clinical Activity of Trametinib in Subjects With Cancer or Plexiform Neurofibromas and Trametinib in Combination With Dabrafenib in Subjects With Cancers Harboring V600 Mutations
NCT02130466	Phase 1/2	COMPLETED	A Study of the Safety and Efficacy of Pembrolizumab (MK-3475) in Combination With Trametinib and Dabrafenib in Participants With Advanced Melanoma (MK-3475-022/KEYNOTE-022)
NCT02143050	Phase 1/2	WITHDRAWN	Study of Dabrafenib, Trametinib and Metformin for Melanoma Patients
NCT02296996	Phase 2	COMPLETED	Dabrafenib and Trametinib for BRAF-inhibitor Pretreated Patients
NCT02314143	Phase 2	TERMINATED	Phase II Biomarker Study Comparing the Combination of BRAF Inhibitor Dabrafenib With MEK Inhibitor Trametinib Versus the Combination After Monotherapy With Dabrafenib or Trametinib
NCT02367859	Phase 2	COMPLETED	Dabrafenib and Trametinib in Treating Patients With BRAF Mutated Ameloblastoma
NCT02392871	Phase 1/2	COMPLETED	Radiotherapy & Combi in Metastatic Melanoma
NCT02410863	Phase 2	TERMINATED	Biopsy- and Biology-driven Optimization of Targeted Therapy in Subjects With Advanced Melanoma
NCT02625337	Phase 2	UNKNOWN	Study Comparing Pembrolizumab With Dual MAPK Pathway Inhibition Plus Pembrolizumab in Melanoma Patients
NCT02672358	Phase 2	WITHDRAWN	Study of Efficacy and Safety of Dabrafenib and Trametinib Combination Therapy in Japanese Patients With BRAF V600E Stage IV NSCLC
NCT02684058	Phase 2	COMPLETED	Study of Efficacy and Safety of Dabrafenib in Combination With Trametinib in Pediatric Patients With BRAF V600 Mutation Positive LGG or Relapsed or Refractory HGG Tumors
NCT02872259	Phase 1/2	COMPLETED	BGB324 in Combination With Pembrolizumab or Dabrafenib/Trametinib in Metastatic Melanoma
NCT02974803	Phase 2	TERMINATED	Concurrent Dabrafenib + Trametinib With Sterotactic Radiation in BRAF Mutation-Positive Malignant Melanoma and Brain Metastases
NCT03239015	Phase 2	UNKNOWN	Efficacy and Safety of Precision Therapy in Refractory Tumor
NCT03244956	Phase 2	COMPLETED	Efficacy of MEK (Trametinib) and BRAFV600E (Dabrafenib) Inhibitors With Radioactive Iodine (RAI) for the Treatment of Refractory Metastatic Differentiated Thyroid Cancer
NCT03352947	Phase 2	COMPLETED	Continuous vs Intermittent Dabrafenib Plus Trametinib in BRAFV600 Mutant Stage 3 Unresectable or Metastatic Melanoma
NCT03391050	Phase 1/2	TERMINATED	A Study of APR-246 in Combination With Dabrafenib in Resistant Patients With BRAF V600 Mutant Melanoma
NCT03455764	Phase 1/2	COMPLETED	MCS110 With BRAF/MEK Inhibition in Patients With Melanoma
NCT03668431	Phase 2	UNKNOWN	Dabrafenib + Trametinib + PDR001 In Colorectal Cancer
NCT03754179	Phase 1/2	UNKNOWN	Dabrafenib/Trametinib/Hydroxychloroquine for Advanced Pretreated BRAF V600 Mutant Melanoma
NCT04059224	Phase 2	COMPLETED	TraMel-WT: A Trial of Trametinib in Patients With Advanced Pretreated BRAFV600 Wild-type Melanoma
NCT04310397	Phase 2	TERMINATED	Dabrafenib, Trametinib, and Spartalizumab for the Treatment of BRAF V600E or V600K Mutation Positive Stage IIIB/C/D Melanoma
NCT04452877	Phase 2	COMPLETED	A Study of Dabrafenib in Combination With Trametinib in Chinese Patients With BRAF V600E Mutant Metastatic NSCLC
NCT04554680	Phase 2	UNKNOWN	Clinical Trial in RAI-Refractory Thyroid Carcinoma Evaluating BRAF & MEK Blockade for Re-differentiation Therapy
NCT04619316	Phase 2	UNKNOWN	Enhancing Radioiodine Incorporation Into Radio Iodine Refractory Thyroid Cancers With MAPK Inhibition
NCT04739566	Phase 2	WITHDRAWN	Dabrafenib and Trametinib Combination as a Neoadjuvant Strategy in BRAF-positive Anaplastic Thyroid Cancer
NCT05182931	Phase 2	UNKNOWN	A Prospective, Multi-Centre Trial of TKI Redifferentiation Therapy in Patients With RAIR Thyroid Cancer (I-FIRST Study)
NCT05299580	Phase 2	WITHDRAWN	Dabrafenib and Trametinib in Circulating Free DNA BRAFV600 Mutated Metastatic Melanoma Patients: a Prospective Phase II, Open Label, Multicentre Study - (Bioliquid TAILOR Study - BIOTAILOR)
NCT05876806	Phase 2	UNKNOWN	Dabrafenib Plus Trametinib in Patients With Advanced Solid Tumor Having BRAF V600E Mutation or Clinically Actionable BRAF Gene Alterations
NCT06362694	Phase 2	UNKNOWN	Study of the Rechallenge Concept in Patients With BRAF-positive Anaplastic Thyroid Cancer After Progression on Anti-BRAF Therapy
NCT01947023	Phase 1	ACTIVE_NOT_RECRUITING	Dabrafenib and Lapatinib in Treating Patients With Refractory Thyroid Cancer That Cannot Be Removed by Surgery
NCT03091257	Phase 1	ACTIVE_NOT_RECRUITING	A Study of Dabrafenib and/or Trametinib in Patients With Relapsed and/or Refractory Multiple Myeloma
NCT03975231	Phase 1	RECRUITING	Dabrafenib, Trametinib, and IMRT in Treating Patients With BRAF Mutated Anaplastic Thyroid Cancer
NCT04903119	Phase 1	RECRUITING	Nilotinib Plus Dabrafenib/Trametinib or Encorafenib/Binimetinib in Metastatic Melanoma
NCT00880321	Phase 1	COMPLETED	A Phase I Study to Investigate the Safety, Pharmacokinetics, and Pharmacodynamics of GSK2118436 in Subjects With Solid Tumors
NCT01231594	Phase 1	COMPLETED	A Rollover Study to Provide Continued Treatment With GSK2118436 to Subjects With BRAF Mutation-Positive Tumors
NCT01262963	Phase 1	COMPLETED	An Absorption, Distribution, Metabolism and Excretion (ADME) Study of Single Oral Dose [14C] GSK2118436 in Subjects With BRAF Mutant Solid Tumors
NCT01340833	Phase 1	COMPLETED	Determination of the Absolute Bioavailability of GSK2118436 Following a Single Oral Dose Co-Administered With an Intravenous Radiolabelled Microtracer of GSK2118436 in Subjects With BRAF Mutant Solid Tumors
NCT01340846	Phase 1	COMPLETED	A Pharmacokinetics Study of the Effects of GSK2118436 on Warfarin, the Effects of Ketoconazole and Gemfibrozil on GSK2118436, and the Effects of Repeat Doses of GSK2118436 in Subjects With BRAF Mutant Solid Tumors
NCT01582997	Phase 1	COMPLETED	A Phase I Study to Investigate the Safety, Tolerability and Pharmacokinetic Profile of of GSK2118436 in Japanese Subjects With BRAF Mutation Positive Solid Tumors
NCT01713972	Phase 1	COMPLETED	Dabrafenib and Pazopanib Hydrochloride in Treating Patients With Advanced Malignant Tumors
NCT01738451	Phase 1	COMPLETED	A Study to Evaluate the Effect of Repeat Oral Dosing of GSK2118436 on Cardiac Repolarization in Subjects With V600 BRAF Mutation-Positive Tumors

Clinical evidence (CIViC)

Variant × therapy × indication — from 99 curated evidence items. CIViC evidence level: A (validated) → B (clinical) → C (case study) → D (preclinical) → E (inferential).

showing 30 of 80 predictive associations by evidence level:

Variant	Therapy	Indication	Effect	Level	CIViC
BRAF V600E	Dabrafenib	Melanoma	Sensitivity/Response	CIViC A	EID11244 +5
BRAF V600E	Trametinib + Dabrafenib	Pleomorphic Xanthoastrocytoma	Sensitivity/Response	CIViC A	EID11312 +1
BRAF V600	Trametinib + Dabrafenib	Skin Melanoma	Sensitivity/Response	CIViC A	EID1411
BRAF V600E	Dabrafenib + Trametinib	Pilocytic Astrocytoma	Sensitivity/Response	CIViC A	EID11313
BRAF V600E	Trametinib + Dabrafenib	Solid Tumor	Sensitivity/Response	CIViC A	EID12161
BRAF V600E	Dabrafenib + Trametinib	Low Grade Glioma	Sensitivity/Response	CIViC A	EID12162
BRAF V600E	Trametinib + Dabrafenib	Lung Non-small Cell Carcinoma	Sensitivity/Response	CIViC A	EID3017
BRAF V600E	Trametinib + Dabrafenib	Anaplastic Thyroid Carcinoma	Sensitivity/Response	CIViC B	EID12959 +3
BRAF V600E	Dabrafenib + Trametinib	Anaplastic Thyroid Carcinoma	Sensitivity/Response	CIViC B	EID12957 +2
BRAF V600E	Trametinib + Dabrafenib	Melanoma	Sensitivity/Response	CIViC B	EID6938 +2
BRAF V600K	Dabrafenib + Trametinib	Melanoma	Sensitivity/Response	CIViC B	EID6939 +2
BRAF V600	Dabrafenib + Trametinib	Melanoma	Sensitivity/Response	CIViC B	EID6180 +1
BRAF V600E	Trametinib + Dabrafenib	Papillary Thyroid Carcinoma	Sensitivity/Response	CIViC B	EID13281 +1
BRAF V600K	Dabrafenib	Melanoma	Sensitivity/Response	CIViC B	EID2505 +1
BRAF K601E	Dabrafenib	Skin Melanoma	Sensitivity/Response	CIViC B	EID2812
BRAF V600	Dabrafenib	Melanoma	Sensitivity/Response	CIViC B	EID1407
BRAF V600	Dabrafenib + Trametinib	Colorectal Cancer	Sensitivity/Response	CIViC B	EID1415
BRAF V600	Dabrafenib	Childhood Low-grade Glioma	Sensitivity/Response	CIViC B	EID8034
BRAF V600D	Dabrafenib	Melanoma	Sensitivity/Response	CIViC B	EID94
BRAF V600E	Dabrafenib	Langerhans-cell Histiocytosis	Sensitivity/Response	CIViC B	EID11303
BRAF V600E	Dabrafenib + Trametinib	Cancer	Sensitivity/Response	CIViC B	EID11672
BRAF V600E	Dabrafenib + Trametinib + Pembrolizumab	Anaplastic Thyroid Carcinoma	Sensitivity/Response	CIViC B	EID13283
BRAF V600E	Dabrafenib	Skin Melanoma	Sensitivity/Response	CIViC B	EID2146
BRAF V600E	Trametinib + Dabrafenib	Skin Melanoma	Sensitivity/Response	CIViC B	EID3758
BRAF V600E	Panitumumab + Dabrafenib + Trametinib	Colorectal Cancer	Sensitivity/Response	CIViC B	EID6123
BRAF V600E	Dabrafenib + Trametinib	Melanoma	Sensitivity/Response	CIViC B	EID6178
BRAF V600E	Trametinib + Dabrafenib	Biliary Tract Cancer	Sensitivity/Response	CIViC B	EID7264
BRAF V600E	Dabrafenib + Trametinib	Cholangiocarcinoma	Sensitivity/Response	CIViC B	EID7453
BRAF V600E	Dabrafenib + Trametinib	Ovarian Cancer	Sensitivity/Response	CIViC B	EID7454
BRAF V600E	Dabrafenib	Papillary Thyroid Carcinoma	Sensitivity/Response	CIViC B	EID7761

CIViC column: a representative evidence item (EID); +N = additional CIViC items supporting the same association.

Pharmacology

MeSH pharmacological classification

MeSH note: An antineoplastic agent that inhibits BRAF kinase.

Pharmacological action: Antineoplastic Agents; Protein Kinase Inhibitors.

Broader MeSH heading: Imidazoles.

MeSH supplementary concept C561627 “dabrafenib” — exact-name match.

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Adverse-event reports (FAERS)

21,087 reports across 2 FAERS drug-name records; 2,339 distinct MedDRA reactions.

openFDA FAERS — spontaneous post-marketing reports. Co-occurrence, not causation: reports are voluntary, unverified, and confounded by indication and reporting bias (the drug’s own indication often appears as a ‘reaction’). PRR is a disproportionality heuristic (reaction rate for this drug vs the FAERS background), NOT a risk estimate. Counts are pooled across the drug’s name records.

Most-reported events

Serious = reports flagged serious (death / life-threatening / hospitalisation / disability / other medically important).

50 reactions by report volume:

Reaction (MedDRA PT)	Reports	Serious	PRR
pyrexia	4,145	3,025 (73%)	12.1×
death	2,882	2,870 (100%)	3.4×
malignant neoplasm progression	1,757	1,751 (100%)	17.6×
fatigue	1,433	850 (59%)	1.8×
nausea	1,406	895 (64%)	1.8×
chills	1,344	821 (61%)	11.6×
rash	1,177	662 (56%)	2.7×
vomiting	983	753 (77%)	2.1×
diarrhoea	982	703 (72%)	1.5×
headache	754	507 (67%)	1.2×
asthenia	735	605 (82%)	1.9×
malaise	622	449 (72%)	1.4×
decreased appetite	589	444 (75%)	2.5×
arthralgia	580	375 (65%)	1.4×
visual impairment	534	224 (42%)	4.4×
product use in unapproved indication	528	354 (67%)	2.2×
pain	505	332 (66%)	0.8×
metastases to central nervous system	496	492 (99%)	40.1×
drug ineffective	483	304 (63%)	0.4×
metastatic malignant melanoma	475	474 (100%)	262.7×
malignant melanoma	435	428 (98%)	33.6×
disease progression	422	332 (79%)	3.6×
dyspnoea	422	355 (84%)	0.8×
dizziness	390	276 (71%)	0.8×
off label use	370	291 (79%)	0.4×
cough	369	273 (74%)	1.3×
dehydration	361	318 (88%)	2.9×
pneumonia	358	354 (99%)	1.1×
vision blurred	338	173 (51%)	2.5×
general physical health deterioration	332	316 (95%)	2.9×
constipation	326	216 (66%)	1.5×
weight decreased	325	264 (81%)	1.2×
hypotension	318	298 (94%)	1.8×
dysphagia	303	194 (64%)	3.2×
pruritus	299	202 (68%)	0.8×
myalgia	296	223 (75%)	1.7×
pain in extremity	290	201 (69%)	1.0×
peripheral swelling	278	195 (70%)	1.8×
anaemia	272	261 (96%)	1.7×
abdominal pain	264	233 (88%)	1.1×
uveitis	263	255 (97%)	19.9×
blood creatine phosphokinase increased	250	241 (96%)	8.6×
confusional state	238	209 (88%)	1.6×
seizure	238	231 (97%)	2.1×
acute kidney injury	232	231 (100%)	1.6×
ejection fraction decreased	231	220 (95%)	15.7×
fall	222	206 (93%)	0.7×
neutropenia	218	216 (99%)	1.6×
infection	217	203 (94%)	1.5×
urinary tract infection	213	191 (90%)	1.3×

Strongest disproportionality

Reactions over-reported for this drug vs the FAERS background (PRR), among those with ≥ 10 reports (a high PRR off a few reports is noise, not signal).

50 reactions by disproportionality:

Reaction (MedDRA PT)	Reports	Serious	PRR
braf v600e mutation positive	27	25 (93%)	890.0×
anaplastic thyroid cancer	49	49 (100%)	663.7×
ganglioglioma	14	14 (100%)	407.2×
metastatic malignant melanoma	475	474 (100%)	262.7×
malignant melanoma stage iv	57	57 (100%)	250.5×
braf gene mutation	15	15 (100%)	197.8×
melanoma recurrent	56	56 (100%)	155.1×
malignant mesenteric neoplasm	10	10 (100%)	152.1×
vogt-koyanagi-harada disease	25	25 (100%)	132.2×
astrocytoma, low grade	12	12 (100%)	75.1×
malignant melanoma stage iii	14	14 (100%)	74.0×
langerhans^ cell histiocytosis	20	20 (100%)	66.1×
serous retinal detachment	46	45 (98%)	61.5×
non-small cell lung cancer recurrent	16	16 (100%)	61.3×
panniculitis	133	130 (98%)	58.4×
sarcoid-like reaction	12	12 (100%)	54.9×
intestinal metastasis	18	18 (100%)	53.9×
metastases to stomach	19	19 (100%)	52.3×
lung adenocarcinoma stage iv	18	18 (100%)	50.0×
acute polyneuropathy	12	12 (100%)	44.8×
glioma	25	25 (100%)	40.7×
skin abrasion	10	9 (90%)	40.2×
metastases to central nervous system	496	492 (99%)	40.1×
cutaneous sarcoidosis	16	16 (100%)	39.3×
metastases to heart	11	11 (100%)	37.6×
thyroid cancer metastatic	10	10 (100%)	36.6×
metastases to skin	35	35 (100%)	35.4×
astrocytoma	13	13 (100%)	34.4×
malignant melanoma	435	428 (98%)	33.6×
small cell carcinoma	11	11 (100%)	33.0×
non-small cell lung cancer stage iv	11	11 (100%)	31.5×
procalcitonin increased	35	35 (100%)	31.2×
keratoacanthoma	20	18 (90%)	30.3×
metastases to spleen	12	12 (100%)	29.9×
chorioretinopathy	41	40 (98%)	29.4×
creatine kinase increased	12	12 (100%)	28.6×
metastases to meninges	60	60 (100%)	27.6×
ureteral disorder	11	11 (100%)	27.3×
detachment of retinal pigment epithelium	23	23 (100%)	27.1×
autoimmune colitis	16	16 (100%)	25.6×
metastases to the mediastinum	10	10 (100%)	24.9×
erythema nodosum	81	73 (90%)	23.8×
tumour invasion	11	11 (100%)	23.6×
hypoalbuminaemia	36	34 (94%)	23.6×
metastases to adrenals	21	21 (100%)	23.4×
palmoplantar keratoderma	15	14 (93%)	21.4×
skin toxicity	111	100 (90%)	20.4×
ocular toxicity	21	19 (90%)	20.4×
uveitis	263	255 (97%)	19.9×
second primary malignancy	133	133 (100%)	19.7×

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.

47 molecules share ≥1 primary target. Top 47 by shared-target count:

Molecule	Source	Status	Shared targets
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	BRAF
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	BRAF
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	BRAF
ABEMACICLIB	ChEMBL	Phase 4 (approved)	BRAF
COBIMETINIB	ChEMBL	Phase 4 (approved)	BRAF
DASATINIB	ChEMBL	Phase 4 (approved)	BRAF
ENCORAFENIB	ChEMBL	Phase 4 (approved)	BRAF
ERLOTINIB	ChEMBL	Phase 4 (approved)	BRAF
FEDRATINIB	ChEMBL	Phase 4 (approved)	BRAF
IMATINIB	ChEMBL	Phase 4 (approved)	BRAF
INFIGRATINIB	ChEMBL	Phase 4 (approved)	BRAF
NILOTINIB	ChEMBL	Phase 4 (approved)	BRAF
PONATINIB	ChEMBL	Phase 4 (approved)	BRAF
RUXOLITINIB	ChEMBL	Phase 4 (approved)	BRAF
SORAFENIB	ChEMBL	Phase 4 (approved)	BRAF
TOVORAFENIB	ChEMBL	Phase 4 (approved)	BRAF
VEMURAFENIB	ChEMBL	Phase 4 (approved)	BRAF
AVUTOMETINIB	ChEMBL	Phase 3	BRAF
MASITINIB	ChEMBL	Phase 3	BRAF
MOTESANIB	ChEMBL	Phase 3	BRAF
NAPORAFENIB	ChEMBL	Phase 3	BRAF
QUERCETIN	ChEMBL	Phase 3	BRAF
BAFETINIB	ChEMBL	Phase 2	BRAF
BELVARAFENIB	ChEMBL	Phase 2	BRAF
BRIMARAFENIB	ChEMBL	Phase 2	BRAF
CEP-32496	ChEMBL	Phase 2	BRAF
DORAMAPIMOD	ChEMBL	Phase 2	BRAF
ELLAGIC ACID	ChEMBL	Phase 2	BRAF
EXARAFENIB	ChEMBL	Phase 2	BRAF
FORETINIB	ChEMBL	Phase 2	BRAF
LIFIRAFENIB	ChEMBL	Phase 2	BRAF
MIRDAMETINIB	ChEMBL	Phase 2	BRAF
PEXMETINIB	ChEMBL	Phase 2	BRAF
R-406	ChEMBL	Phase 2	BRAF
RAF-265	ChEMBL	Phase 2	BRAF
REBASTINIB	ChEMBL	Phase 2	BRAF
TG100-115	ChEMBL	Phase 2	BRAF
TINLORAFENIB	ChEMBL	Phase 2	BRAF
XL-281	ChEMBL	Phase 2	BRAF
Afatinib	PubChem	Approved	BRAF
Binimetinib	PubChem	Approved	BRAF
Crizotinib	PubChem	Approved	BRAF
dacomitinib	PubChem	Approved	BRAF
Fostamatinib	PubChem	Approved	BRAF
Idelalisib	PubChem	Approved	BRAF
Selumetinib	PubChem	Approved	BRAF
Trametinib	PubChem	Approved	BRAF