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:

Property	Value	Reference
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
CL (Clearance)	2.86 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.60 hours	Lombardo F, Berellini G, Obach RS

Approvals:

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

FDA Adverse Event Reporting System (Female)

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
Blood creatine phosphokinase increased	84.25	20.25	64	14666	30366	63443926
Drug ineffective	83.99	20.25	72	14658	1044693	62429599
Product use in unapproved indication	80.67	20.25	147	14583	178933	63295359
Erythema nodosum	76.13	20.25	32	14698	4843	63469449
Vision blurred	76.06	20.25	100	14630	91824	63382468
Serous retinal detachment	67.87	20.25	16	14714	351	63473941
Dermatitis acneiform	62.35	20.25	28	14702	4968	63469324
Skin toxicity	57.50	20.25	26	14704	4688	63469604
Metastatic malignant melanoma	55.71	20.25	18	14712	1297	63472995
Second primary malignancy	55.53	20.25	30	14700	7923	63466369
Nausea	52.72	20.25	358	14372	854113	62620179
Vogt-Koyanagi-Harada disease	51.79	20.25	11	14719	147	63474145
Off label use	50.98	20.25	49	14681	674413	62799879
Hyperpyrexia	50.63	20.25	22	14708	3610	63470682
Chorioretinopathy	50.37	20.25	15	14715	824	63473468
Drug hypersensitivity	48.90	20.25	7	14723	310680	63163612
Iridocyclitis	47.72	20.25	19	14711	2503	63471789
Vomiting	44.80	20.25	251	14479	559366	62914926
Condition aggravated	44.27	20.25	19	14711	402198	63072094
Metastasis	43.11	20.25	22	14708	5175	63469117
Malignant melanoma	40.83	20.25	28	14702	11328	63462964
Metastases to lung	40.18	20.25	29	14701	12721	63461571
Haemophagocytic lymphohistiocytosis	40.11	20.25	27	14703	10600	63463692
Blood lactate dehydrogenase increased	39.86	20.25	37	14693	23079	63451213
BRAF V600E mutation positive	39.39	20.25	7	14723	33	63474259
Erythema multiforme	38.77	20.25	26	14704	10143	63464149
Rash maculo-papular	38.36	20.25	42	14688	31854	63442438
Cutaneous sarcoidosis	37.75	20.25	10	14720	357	63473935
Metastases to meninges	37.05	20.25	16	14714	2586	63471706
Melanoma recurrent	35.17	20.25	8	14722	149	63474143
Dehydration	35.16	20.25	104	14626	173250	63301042
Hyperkeratosis	34.65	20.25	20	14710	5998	63468294
Palmar-plantar erythrodysaesthesia syndrome	34.31	20.25	34	14696	22981	63451311
Sinusitis	33.64	20.25	6	14724	226647	63247645
Rhabdomyolysis	33.54	20.25	46	14684	43905	63430387
Non-small cell lung cancer recurrent	33.28	20.25	7	14723	89	63474203
Systemic inflammatory response syndrome	33.21	20.25	19	14711	5602	63468690
Abdominal discomfort	32.45	20.25	17	14713	320868	63153424
Aspartate aminotransferase increased	31.92	20.25	67	14663	90210	63384082
Arthropathy	31.20	20.25	8	14722	234784	63239508
Myalgia	30.75	20.25	89	14641	146440	63327852
Vitreous floaters	29.57	20.25	18	14712	5948	63468344
Retinal detachment	29.56	20.25	18	14712	5951	63468341
Pneumonitis	28.60	20.25	38	14692	35184	63439108
Discomfort	28.19	20.25	3	14727	167371	63306921
Treatment failure	26.03	20.25	7	14723	199036	63275256
Panniculitis lobular	25.98	20.25	5	14725	39	63474253
Squamous cell carcinoma	25.76	20.25	19	14711	8613	63465679
Paronychia	25.57	20.25	16	14714	5549	63468743
Fall	24.66	20.25	33	14697	392301	63081991
Decreased appetite	23.68	20.25	118	14612	250934	63223358
Dry skin	23.43	20.25	45	14685	56842	63417450
Alanine aminotransferase increased	22.70	20.25	64	14666	103706	63370586
Hyperthermia	22.60	20.25	18	14712	9138	63465154
Leukoderma	22.53	20.25	5	14725	83	63474209
Hepatitis	22.25	20.25	36	14694	39752	63434540
Joint swelling	22.21	20.25	26	14704	327640	63146652
Keratoacanthoma	22.06	20.25	7	14723	476	63473816
Swelling	21.92	20.25	19	14711	275359	63198933
Sarcoid-like reaction	21.56	20.25	4	14726	25	63474267
Acute polyneuropathy	21.55	20.25	6	14724	259	63474033
Immune-mediated hepatitis	21.41	20.25	9	14721	1362	63472930
Metastatic neoplasm	21.39	20.25	13	14717	4282	63470010
Hypersensitivity	21.18	20.25	22	14708	292663	63181629
Electrocardiogram QT prolonged	20.83	20.25	44	14686	59486	63414806
Weight increased	20.75	20.25	18	14712	260774	63213518
Gamma-glutamyltransferase increased	20.70	20.25	32	14698	33999	63440293
Infective glossitis	20.27	20.25	4	14726	36	63474256

FDA Adverse Event Reporting System (Male)

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
Product use in unapproved indication	76.25	18.31	166	15696	117333	34823736
Off label use	75.50	18.31	49	15813	419475	34521594
Metastases to stomach	72.99	18.31	15	15847	79	34940990
Rash	70.99	18.31	242	15620	222510	34718559
Blood creatine phosphokinase increased	70.35	18.31	94	15768	44763	34896306
Basal cell carcinoma	69.17	18.31	63	15799	19595	34921474
Metastases to lung	65.69	18.31	45	15817	9275	34931794
Squamous cell carcinoma	61.67	18.31	47	15815	11428	34929641
Hyperpyrexia	56.93	18.31	27	15835	2761	34938308
Melanoma recurrent	55.18	18.31	13	15849	139	34940930
Metastatic malignant melanoma	54.90	18.31	24	15838	2031	34939038
Chorioretinopathy	51.80	18.31	21	15841	1472	34939597
Malignant melanoma	49.90	18.31	36	15826	8054	34933015
Fatigue	49.02	18.31	311	15551	370342	34570727
Haemophagocytic lymphohistiocytosis	48.44	18.31	43	15819	12930	34928139
Metastases to peritoneum	47.53	18.31	21	15841	1823	34939246
Blood lactate dehydrogenase increased	46.93	18.31	55	15807	22935	34918134
Panniculitis	45.95	18.31	21	15841	1973	34939096
Metastases to skin	45.34	18.31	14	15848	438	34940631
C-reactive protein increased	44.00	18.31	84	15778	54014	34887055
Vision blurred	43.23	18.31	76	15786	45887	34895182
Erythema nodosum	42.91	18.31	18	15844	1376	34939693
Drug interaction	42.44	18.31	25	15837	225921	34715148
Metastases to meninges	42.18	18.31	18	15844	1436	34939633
Hyperkeratosis	41.24	18.31	24	15838	3725	34937344
Serous retinal detachment	41.17	18.31	14	15848	598	34940471
Metastases to lymph nodes	41.03	18.31	26	15836	4702	34936367
Malignant mesenteric neoplasm	38.64	18.31	8	15854	44	34941025
Metastases to bone	37.55	18.31	36	15826	11934	34929135
Procalcitonin increased	35.88	18.31	17	15845	1734	34939335
Metastasis	34.00	18.31	22	15840	4122	34936947
Jejunal ulcer perforation	33.92	18.31	8	15854	86	34940983
Toxicity to various agents	32.50	18.31	26	15836	200336	34740733
Drug ineffective	31.19	18.31	105	15757	456646	34484423
Decreased appetite	30.75	18.31	153	15709	166239	34774830
Intestinal metastasis	30.27	18.31	9	15853	247	34940822
Metastases to heart	29.94	18.31	8	15854	147	34940922
Omental necrosis	29.46	18.31	6	15856	30	34941039
Nausea	29.31	18.31	258	15604	339650	34601419
Tissue infiltration	29.21	18.31	7	15855	81	34940988
Mesenteric neoplasm	29.13	18.31	6	15856	32	34941037
Gastrointestinal wall thickening	29.04	18.31	14	15848	1484	34939585
Brain neoplasm	28.73	18.31	18	15844	3191	34937878
Ureteral disorder	28.33	18.31	8	15854	182	34940887
Eastern Cooperative Oncology Group performance status	28.12	18.31	6	15856	39	34941030
Vomiting	25.64	18.31	196	15666	247425	34693644
Anxiety	25.12	18.31	7	15855	99421	34841648
Anaplastic thyroid cancer	24.56	18.31	4	15858	3	34941066
Disease progression	24.08	18.31	105	15757	107972	34833097
Overdose	23.78	18.31	6	15856	91053	34850016
Papilloedema	23.74	18.31	15	15847	2698	34938371
Concomitant disease aggravated	23.50	18.31	20	15842	5681	34935388
Condition aggravated	23.22	18.31	32	15830	192164	34748905
General physical health deterioration	23.01	18.31	117	15745	128152	34812917
Retinal detachment	22.40	18.31	19	15843	5372	34935697
Epilepsy	22.11	18.31	37	15825	21458	34919611
Iridocyclitis	22.03	18.31	12	15850	1640	34939429
Influenza like illness	21.34	18.31	42	15820	27592	34913477
Metastases to adrenals	21.27	18.31	10	15852	1002	34940067
BRAF gene mutation	21.09	18.31	5	15857	55	34941014
Bacterial diarrhoea	20.85	18.31	5	15857	58	34941011
Depression	20.80	18.31	9	15853	97089	34843980
Tumour invasion	20.45	18.31	7	15855	305	34940764
Brain neoplasm malignant	19.70	18.31	9	15853	845	34940224
Abdominal lymphadenopathy	19.70	18.31	9	15853	845	34940224
Febrile neutropenia	19.49	18.31	20	15842	136829	34804240
Leukoderma	19.48	18.31	5	15857	78	34940991
Body temperature fluctuation	19.21	18.31	11	15851	1656	34939413
General physical condition abnormal	19.18	18.31	15	15847	3784	34937285
Liver function test increased	19.05	18.31	28	15834	14537	34926532
Cerebral haemorrhage	18.89	18.31	46	15816	34891	34906178
Small intestine carcinoma	18.84	18.31	8	15854	630	34940439
Asthenia	18.48	18.31	181	15681	245070	34695999
Hypophysitis	18.42	18.31	12	15850	2274	34938795

FDA Adverse Event Reporting System (Geriatric)

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
Squamous cell carcinoma	104.27	17.63	63	24353	15559	79704413
Second primary malignancy	103.93	17.63	61	24355	14289	79705683
Erythema nodosum	99.44	17.63	43	24373	5274	79714698
Serous retinal detachment	97.84	17.63	28	24388	1006	79718966
Hyperpyrexia	96.98	17.63	44	24372	6048	79713924
Chorioretinopathy	95.67	17.63	33	24383	2198	79717774
Blood lactate dehydrogenase increased	95.53	17.63	86	24330	39084	79680888
Haemophagocytic lymphohistiocytosis	94.17	17.63	67	24349	21770	79698202
Basal cell carcinoma	87.11	17.63	80	24336	37295	79682677
Metastases to liver	87.06	17.63	71	24345	28243	79691729
Metastases to lung	81.27	17.63	57	24359	18106	79701866
Drug ineffective	81.26	17.63	129	24287	1080784	78639188
Rash	80.50	17.63	370	24046	577988	79141984
Malignant melanoma	77.22	17.63	51	24365	14690	79705282
Metastatic malignant melanoma	76.88	17.63	30	24386	2833	79717139
Dermatitis acneiform	71.10	17.63	42	24374	9951	79710021
Metastasis	68.32	17.63	36	24380	6844	79713128
Melanoma recurrent	68.22	17.63	16	24400	256	79719716
Hyperkeratosis	66.85	17.63	37	24379	7753	79712219
Iridocyclitis	66.15	17.63	29	24387	3675	79716297
Condition aggravated	64.09	17.63	37	24379	501087	79218885
C-reactive protein increased	63.33	17.63	129	24287	128898	79591074
Product use in unapproved indication	62.15	17.63	193	24223	250166	79469806
Metastases to stomach	61.93	17.63	15	24401	277	79719695
Metastases to meninges	60.47	17.63	27	24389	3574	79716398
Visual impairment	58.72	17.63	103	24313	92028	79627944
Procalcitonin increased	58.48	17.63	25	24391	2981	79716991
Drug hypersensitivity	57.35	17.63	11	24405	298905	79421067
Metastases to lymph nodes	56.97	17.63	37	24379	10360	79709612
Skin toxicity	56.69	17.63	34	24382	8280	79711692
Metastases to bone	54.42	17.63	51	24365	24376	79695596
BRAF V600E mutation positive	54.07	17.63	10	24406	44	79719928
Rash maculo-papular	51.34	17.63	74	24342	56004	79663968
Cutaneous sarcoidosis	50.15	17.63	14	24402	459	79719513
Rheumatoid arthritis	48.82	17.63	4	24412	208466	79511506
Vogt-Koyanagi-Harada disease	48.79	17.63	12	24404	237	79719735
Drug interaction	48.46	17.63	34	24382	415149	79304823
Retinal detachment	48.45	17.63	32	24384	9215	79710757
Decreased appetite	46.69	17.63	218	24198	342200	79377772
Metastases to peritoneum	46.62	17.63	24	24392	4348	79715624
Metastases to skin	45.91	17.63	18	24398	1721	79718251
Vomiting	44.57	17.63	352	24064	665476	79054496
Aspartate aminotransferase increased	44.19	17.63	117	24299	138524	79581448
Vision blurred	42.91	17.63	98	24318	105800	79614172
Toxicity to various agents	42.37	17.63	40	24376	421500	79298472
Dehydration	42.25	17.63	169	24247	248018	79471954
Malignant mesenteric neoplasm	40.50	17.63	8	24408	53	79719919
BRAF gene mutation	39.75	17.63	8	24408	59	79719913
Detachment of retinal pigment epithelium	38.63	17.63	13	24403	803	79719169
Squamous cell carcinoma of skin	36.57	17.63	32	24384	14001	79705971
Metastases to adrenals	35.94	17.63	14	24402	1316	79718656
Demyelinating polyneuropathy	35.72	17.63	15	24401	1711	79718261
Blood alkaline phosphatase increased	35.26	17.63	67	24349	63597	79656375
Overdose	34.84	17.63	7	24409	184199	79535773
Intestinal metastasis	34.50	17.63	10	24406	376	79719596
Jejunal ulcer perforation	34.41	17.63	8	24408	123	79719849
Sinusitis	33.86	17.63	9	24407	195492	79524480
Pneumonitis	33.65	17.63	64	24352	60796	79659176
Therapeutic product effect incomplete	32.39	17.63	3	24413	141642	79578330
Anxiety	32.21	17.63	18	24398	248494	79471478
Palmar-plantar erythrodysaesthesia syndrome	32.21	17.63	45	24371	33089	79686883
Keratoacanthoma	31.82	17.63	12	24404	1033	79718939
Nausea	31.09	17.63	437	23979	956759	78763213
Hypophysitis	30.93	17.63	18	24398	4148	79715824
Musculoskeletal stiffness	30.41	17.63	8	24408	175000	79544972
Concomitant disease aggravated	30.31	17.63	28	24388	13139	79706833
Hepatocellular injury	30.04	17.63	53	24363	47540	79672432
Rhabdomyolysis	29.82	17.63	84	24332	103047	79616925
Omental necrosis	29.72	17.63	6	24410	45	79719927
Gamma-glutamyltransferase increased	29.61	17.63	57	24359	54623	79665349
Joint swelling	29.44	17.63	27	24389	288619	79431353
Non-small cell lung cancer recurrent	29.34	17.63	7	24409	121	79719851
Eastern Cooperative Oncology Group performance status	29.16	17.63	6	24410	50	79719922
Abdominal lymphadenopathy	28.98	17.63	12	24404	1322	79718650
Disease progression	28.56	17.63	122	24294	184240	79535732
General physical health deterioration	28.27	17.63	162	24254	275076	79444896
Weight increased	28.22	17.63	26	24390	277360	79442612
Product dose omission issue	27.90	17.63	21	24395	247516	79472456
Alanine aminotransferase increased	27.88	17.63	111	24305	162459	79557513
Blood pressure increased	27.84	17.63	15	24401	211345	79508627
Mesenteric neoplasm	27.66	17.63	6	24410	66	79719906
Hypersensitivity	27.37	17.63	24	24392	262215	79457757
Arthropathy	27.36	17.63	10	24406	177101	79542871
Lipase increased	26.79	17.63	29	24387	16437	79703535
Autoimmune colitis	26.71	17.63	12	24404	1611	79718361
Gastrointestinal wall thickening	26.65	17.63	14	24402	2643	79717329
Papilloedema	26.58	17.63	19	24397	6214	79713758
Visual acuity reduced	25.68	17.63	38	24378	29431	79690541
Asthenia	25.60	17.63	254	24162	511435	79208537
Tumour invasion	25.56	17.63	8	24408	392	79719580
Abdominal discomfort	24.92	17.63	24	24392	250703	79469269
Paronychia	24.88	17.63	20	24396	7788	79712184
Hyperthermia	24.63	17.63	29	24387	18008	79701964
Intentional product use issue	24.51	17.63	8	24408	152104	79567868
Myalgia	24.38	17.63	117	24299	185524	79534448
Metastases to heart	23.54	17.63	7	24409	288	79719684
Fatigue	23.48	17.63	407	24009	929320	78790652
Influenza like illness	23.32	17.63	61	24355	71646	79648326
Nasopharyngitis	23.31	17.63	26	24390	253855	79466117
Cerebral haemorrhage	22.94	17.63	53	24363	57620	79662352
Fall	22.78	17.63	75	24341	487554	79232418
Ureteral disorder	22.74	17.63	8	24408	565	79719407
Disseminated intravascular coagulation	22.73	17.63	40	24376	35802	79684170
Insomnia	22.63	17.63	25	24391	245145	79474827
Intentional overdose	22.32	17.63	3	24413	105957	79614015
Therapy partial responder	22.16	17.63	27	24389	17370	79702602
Body temperature fluctuation	21.97	17.63	14	24402	3793	79716179
Vitreous floaters	21.89	17.63	18	24398	7238	79712734
Erythema multiforme	21.85	17.63	27	24389	17624	79702348
Treatment failure	21.16	17.63	13	24403	170473	79549499
Erysipelas	21.05	17.63	21	24395	10829	79709143
Vitiligo	20.84	17.63	11	24405	2098	79717874
Metastatic neoplasm	20.66	17.63	15	24401	5027	79714945
Dyspnoea	20.13	17.63	167	24249	856858	78863114
Swelling	20.11	17.63	22	24394	216689	79503283
Acute polyneuropathy	20.05	17.63	7	24409	483	79719489
Left ventricular dysfunction	19.87	17.63	27	24389	19334	79700638
Brain oedema	19.78	17.63	31	24385	25232	79694740
Macular oedema	19.55	17.63	15	24401	5459	79714513
Sarcoid-like reaction	19.07	17.63	4	24412	37	79719935
Epilepsy	19.02	17.63	40	24376	40820	79679152
Therapy cessation	18.93	17.63	38	24378	37524	79682448
Hepatitis	18.73	17.63	48	24368	55679	79664293
Amylase increased	18.69	17.63	20	24396	11189	79708783
Peripheral motor neuropathy	18.49	17.63	12	24404	3355	79716617
Serous retinopathy	18.15	17.63	5	24411	156	79719816
Small intestine carcinoma	18.14	17.63	8	24408	1028	79718944
Liver disorder	18.08	17.63	56	24360	72361	79647611
Panniculitis lobular	18.05	17.63	4	24412	49	79719923
Chest discomfort	17.87	17.63	10	24406	138034	79581938
Transaminases increased	17.84	17.63	45	24371	51698	79668274
Leukoderma	17.76	17.63	5	24411	169	79719803
Tissue infiltration	17.71	17.63	7	24409	684	79719288
Cholestasis	17.63	17.63	45	24371	52064	79667908

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EC02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS B-Raf serine-threonine kinase (BRAF) inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
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
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190107	Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA	N0000190108	Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA	N0000190110	Organic Anion Transporter 1 Inhibitors
FDA MoA	N0000190111	Organic Anion Transporter 3 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:75047	BRAF inhibitors
CHEBI has role	CHEBI:149553	anticoronaviral drug

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

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

🐶 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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
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 75MG 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 75MG 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 75MG 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 75MG 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 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 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
EQ 75MG 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 75MG 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 75MG 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 75MG 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
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	7994185	Jan. 20, 2030	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	7994185	Jan. 20, 2030	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	7994185	Jan. 20, 2030	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	7994185	Jan. 20, 2030	TREATMENT OF MELANOMA
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8415345	Jan. 20, 2030	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	8415345	Jan. 20, 2030	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	8415345	Jan. 20, 2030	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	8415345	Jan. 20, 2030	TREATMENT OF MELANOMA
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	7994185	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	7994185	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	7994185	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	7994185	Jan. 20, 2030	TREATMENT OF MELANOMA
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8415345	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8415345	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8415345	Jan. 20, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8415345	Jan. 20, 2030	TREATMENT OF MELANOMA
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	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	8703781	Oct. 15, 2030	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	8703781	Oct. 15, 2030	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	8952018	Oct. 15, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8703781	Oct. 15, 2030	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	8952018	Oct. 15, 2030	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 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	10869869	Aug. 30, 2033	TAFINLAR(R) 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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	10869869	Aug. 30, 2033	TAFINLAR(R) 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

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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 75MG 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 75MG 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 75MG 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 75MG 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 75MG 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 75MG 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 75MG 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
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	March 16, 2026	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	March 16, 2026	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 10MG BASE	TAFINLAR	NOVARTIS	N217514	March 16, 2023	RX	TABLET, FOR SUSPENSION	ORAL	March 16, 2026	NEW PRODUCT
EQ 50MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	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 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	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 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

Bioactivity Summary:

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
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	6.07	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	5.79	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	5.87	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	7.48	CHEMBL
Cyclin-dependent-like kinase 5	Kinase	Q00535	CDK5_HUMAN		Kd	5.97	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	6.28	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	6.52	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.81	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	6.14	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		IC50	7.11	CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	7.89	CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	6.22	CHEMBL
TGF-beta receptor type-2	Kinase	P37173	TGFR2_HUMAN		Kd	5.60	CHEMBL
Cyclin-dependent kinase 6	Kinase	Q00534	CDK6_HUMAN		Kd	6.50	CHEMBL
Protein-tyrosine kinase 6	Kinase	Q13882	PTK6_HUMAN		Kd	5.85	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	7.18	CHEMBL
Cyclin-dependent kinase 17	Kinase	Q00537	CDK17_HUMAN		Kd	7.44	CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	6.74	CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	7.09	CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.74	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	6.19	CHEMBL
Calcium/calmodulin-dependent protein kinase type IV	Kinase	Q16566	KCC4_HUMAN		Kd	5.64	CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	6	CHEMBL
Serine/threonine-protein kinase Nek9	Kinase	Q8TD19	NEK9_HUMAN		Kd	7.28	CHEMBL
TGF-beta receptor type-1	Kinase	P36897	TGFR1_HUMAN		IC50	5.43	CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	6.15	CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	7.47	CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	6.92	CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		IC50	4.27	CHEMBL
Cyclin-dependent kinase 4	Kinase	P11802	CDK4_HUMAN		Kd	6.90	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	6.38	CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1	Kinase	O75460	ERN1_HUMAN		Kd	5.84	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	5.81	CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6.73	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.83	CHEMBL
Serine/threonine-protein kinase SIK3	Kinase	Q9Y2K2	SIK3_HUMAN		Kd	5.70	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1	Kinase	Q9BQI3	E2AK1_HUMAN		Kd	6.02	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	5.64	CHEMBL
Dual serine/threonine and tyrosine protein kinase	Kinase	Q6XUX3	DUSTY_HUMAN		IC50	4.53	CHEMBL
Serine/threonine-protein kinase A-Raf	Kinase	P10398	ARAF_HUMAN		IC50	7.59	CHEMBL
GTPase KRas	Enzyme	P01116	RASK_HUMAN		IC50	5.23	CHEMBL
Serine/threonine-protein kinase Nek1	Kinase	Q96PY6	NEK1_HUMAN		Kd	6.32	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		IC50	8.70	CHEMBL
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN		EC50	7.06	CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE2	Kinase	Q76MJ5	ERN2_HUMAN		Kd	6.94	CHEMBL

External reference:

ID	Source
D10064	KEGG_DRUG
1195768-06-9	SECONDARY_CAS_RN
4032496	VANDF
CHEBI:75045	CHEBI
P06	PDB_CHEM_ID
CHEMBL2028663	ChEMBL_ID
CHEMBL2105729	ChEMBL_ID
C561627	MESH_SUPPLEMENTAL_RECORD_UI
6494	IUPHAR_LIGAND_ID
9458	INN_ID
DB08912	DRUGBANK_ID
QGP4HA4G1B	UNII
1424911	RXNORM
203107	MMSL
29476	MMSL
29650	MMSL
d08103	MMSL
015042	NDDF
015043	NDDF
703641001	SNOMEDCT_US
703642008	SNOMEDCT_US
703646006	SNOMEDCT_US
C3467876	UMLSCUI
CHEMBL523411	ChEMBL_ID
44462760	PUBCHEM_CID

Pharmaceutical products:

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