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dabrafenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors	4801	1195765-45-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GSK2118436B dabrafenib mesylate tafinlar dabrafenib GSK2118436 dabrafenib mesilate	Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo. Molecular weight: 519.56 Formula: C23H20F3N5O2S2 CLOGP: 4.76 LIPINSKI: 1 HAC: 7 HDO: 2 TPSA: 110.86 ALOGS: -5.20 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GSK2118436B
dabrafenib mesylate
tafinlar
dabrafenib
GSK2118436
dabrafenib mesilate

Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

Molecular weight: 519.56
Formula: C23H20F3N5O2S2
CLOGP: 4.76
LIPINSKI: 1
HAC: 7
HDO: 2
TPSA: 110.86
ALOGS: -5.20
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	2.86 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.60 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.65 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
Aug. 26, 2013	EMA	Novartis Europharm Limited
March 28, 2016	PMDA	Novartis Pharma K.K.
May 29, 2013	FDA	NOVARTIS PHARMS CORP

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1446.13	20.25	1041	13689	469437	63004855
Malignant neoplasm progression	841.73	20.25	400	14330	81721	63392571
Chills	413.10	20.25	281	14449	113097	63361195
Death	285.74	20.25	390	14340	373991	63100301
Uveitis	263.96	20.25	102	14628	12451	63461841
Metastases to central nervous system	249.18	20.25	99	14631	13006	63461286
Visual impairment	161.35	20.25	143	14587	84303	63389989
Panniculitis	139.59	20.25	63	14667	11322	63462970
Ejection fraction decreased	120.18	20.25	71	14659	22261	63452031
Rash	89.46	20.25	309	14421	560562	62913730

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1399.05	18.31	1165	14697	331848	34609221
Malignant neoplasm progression	749.43	18.31	476	15386	87570	34853499
Chills	438.06	18.31	332	15530	80711	34860358
Metastases to central nervous system	416.24	18.31	152	15710	8053	34933016
Death	242.91	18.31	546	15316	397503	34543566
Ejection fraction decreased	191.05	18.31	115	15747	19039	34922030
Uveitis	141.88	18.31	69	15793	7466	34933603
Visual impairment	113.10	18.31	108	15754	35694	34905375
Metastases to liver	96.41	18.31	66	15796	13597	34927472
Second primary malignancy	77.68	18.31	47	15815	7839	34933230

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	2116.98	17.63	1695	22721	677014	79042958
Malignant neoplasm progression	1238.45	17.63	669	23747	135321	79584651
Chills	559.85	17.63	432	23984	159802	79560170
Metastases to central nervous system	477.37	17.63	182	24234	16193	79703779
Death	357.74	17.63	628	23788	565886	79154086
Uveitis	327.82	17.63	140	24276	16690	79703282
Ejection fraction decreased	315.85	17.63	171	24245	34406	79685566
Blood creatine phosphokinase increased	151.32	17.63	140	24276	65950	79654022
Panniculitis	138.05	17.63	70	24346	12301	79707671
Off label use	105.42	17.63	75	24341	907140	78812832

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EC02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS B-Raf serine-threonine kinase (BRAF) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:75047	BRAF inhibitors
CHEBI has role	CHEBI:149553	anticoronaviral drug
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors
FDA MoA	N0000185506	Cytochrome P450 3A4 Inducers
FDA MoA	N0000185507	Cytochrome P450 2C9 Inducers
FDA MoA	N0000185607	Cytochrome P450 2C19 Inducers
FDA MoA	N0000187063	Cytochrome P450 2C8 Inducers

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Metastatic malignant melanoma	indication	443493003
Malignant Melanoma with BRAF V600E Mutation	indication	830150003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.56	acidic
pKa2	3.35	Basic
pKa3	0.43	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 10MG BASE	TAFINLAR	NOVARTIS	N217514	March 16, 2023	RX	TABLET, FOR SUSPENSION	ORAL	8835443	June 10, 2025	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 10MG BASE	TAFINLAR	NOVARTIS	N217514	March 16, 2023	RX	TABLET, FOR SUSPENSION	ORAL	8703781	Oct. 15, 2030	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8835443	June 10, 2025	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8835443	June 10, 2025	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8835443	June 10, 2025	TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8835443	June 10, 2025	TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	9233956	May 4, 2029	TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	9233956	May 4, 2029	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	9233956	May 4, 2029	TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	9233956	May 4, 2029	TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	TAFINLAR	NOVARTIS	N217514	March 16, 2023	RX	TABLET, FOR SUSPENSION	ORAL	March 16, 2026	NEW PRODUCT
EQ 10MG BASE	TAFINLAR	NOVARTIS	N217514	March 16, 2023	RX	TABLET, FOR SUSPENSION	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	June 22, 2024	DABRAFENIB IN COMBINATION WITH TRAMETINIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Dec. 22, 2024	PEDIATRIC EXCLUSIVITY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	April 30, 2025	TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	May 4, 2025	TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	June 22, 2025	DABRAFENIB IS INDICATED IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Oct. 30, 2025	PEDIATRIC EXCLUSIVITY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Nov. 4, 2025	PEDIATRIC EXCLUSIVITY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN	INHIBITOR	IC50	9.16	WOMBAT-PK	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	5.81	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	6.11	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	5.89	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	6.09	CHEMBL
RAF proto-oncogene serine/threonine-protein kinase	Kinase	P04049	RAF1_HUMAN		IC50	6.82	CHEMBL
Cyclin-dependent kinase 1	Kinase	P06493	CDK1_HUMAN		Kd	6.44	CHEMBL
Cyclin-dependent kinase 2	Kinase	P24941	CDK2_HUMAN		Kd	7.72	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.78	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	5.49	CHEMBL

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External reference:

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ID	Source
P06	PDB_CHEM_ID
015042	NDDF
015043	NDDF
1195768-06-9	SECONDARY_CAS_RN
1424911	RXNORM
203107	MMSL
29476	MMSL
29650	MMSL
4032496	VANDF
44462760	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	33 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1154	TABLET, FOR SUSPENSION	10 mg	ORAL	NDA	33 sections

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