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: ONP 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: ONP

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	1313.59	20.70	919	11373	379284	50213548
Malignant neoplasm progression	705.52	20.70	339	11953	67785	50525047
Chills	345.58	20.70	241	12051	96446	50496386
Uveitis	240.43	20.70	89	12203	9221	50583611
Metastases to central nervous system	227.30	20.70	90	12202	11192	50581640
Death	201.88	20.70	315	11977	325064	50267768
Panniculitis	127.69	20.70	55	12237	8448	50584384
Ejection fraction decreased	102.66	20.70	61	12231	18459	50574373
Visual impairment	89.41	20.70	96	12196	68179	50524653
Rash	73.62	20.70	253	12039	437218	50155614
Blood creatine phosphokinase increased	69.77	20.70	55	12237	26312	50566520
Erythema nodosum	67.77	20.70	28	12264	3875	50588957
Dermatitis acneiform	66.73	20.70	28	12264	4029	50588803
Drug ineffective	66.67	20.70	61	12231	819272	49773560
Serous retinal detachment	52.14	20.70	12	12280	225	50592607
Chorioretinopathy	49.92	20.70	15	12277	811	50592021
Vogt-Koyanagi-Harada disease	47.93	20.70	10	12282	116	50592716
Second primary malignancy	46.93	20.70	26	12266	6888	50585944
Hyperpyrexia	43.40	20.70	19	12273	3030	50589802
Vision blurred	42.75	20.70	72	12220	78575	50514257
Product use in unapproved indication	41.79	20.70	89	12203	115730	50477102
Drug hypersensitivity	41.18	20.70	6	12286	251004	50341828
Metastatic malignant melanoma	40.81	20.70	14	12278	1160	50591672
Erythema multiforme	40.45	20.70	26	12266	9024	50583808
Metastases to meninges	40.39	20.70	16	12276	1986	50590846
Iridocyclitis	40.03	20.70	16	12276	2033	50590799
BRAF V600E mutation positive	39.81	20.70	7	12285	29	50592803
Rash maculo-papular	39.38	20.70	40	12252	26601	50566231
Melanoma recurrent	38.57	20.70	8	12284	90	50592742
Malignant melanoma	37.84	20.70	26	12266	10082	50582750
Vomiting	37.72	20.70	215	12077	460543	50132289
Metastasis	36.87	20.70	19	12273	4356	50588476
Nausea	36.70	20.70	294	11998	705104	49887728
Skin toxicity	35.90	20.70	18	12274	3895	50588937
Hyperkeratosis	34.36	20.70	19	12273	5016	50587816
Blood lactate dehydrogenase increased	33.81	20.70	32	12260	19530	50573302
Cutaneous sarcoidosis	33.76	20.70	9	12283	314	50592518
Off label use	33.15	20.70	40	12252	474386	50118446
Rhabdomyolysis	31.54	20.70	43	12249	38984	50553848
Metastases to lung	31.34	20.70	24	12268	10996	50581836
Dehydration	30.73	20.70	94	12198	152355	50440477
Condition aggravated	30.70	20.70	17	12275	297041	50295791
Systemic inflammatory response syndrome	28.93	20.70	17	12275	5032	50587800
Myalgia	28.24	20.70	80	12212	124239	50468593
Aspartate aminotransferase increased	28.18	20.70	60	12232	77938	50514894
Vitreous floaters	28.13	20.70	17	12275	5297	50587535
Palmar-plantar erythrodysaesthesia syndrome	27.58	20.70	29	12263	20069	50572763
Squamous cell carcinoma	26.84	20.70	19	12273	7720	50585112
Pneumonitis	26.13	20.70	34	12258	29476	50563356
Retinal detachment	26.10	20.70	16	12276	5113	50587719
Sinusitis	25.91	20.70	5	12287	170553	50422279
C-reactive protein increased	23.85	20.70	51	12241	66423	50526409
Abdominal discomfort	22.86	20.70	14	12278	231627	50361205
Decreased appetite	22.86	20.70	103	12189	200820	50392012
Haemophagocytic lymphohistiocytosis	22.81	20.70	18	12274	8615	50584217
Keratoacanthoma	22.61	20.70	7	12285	419	50592413
Leukoderma	22.53	20.70	5	12287	79	50592753
Acute polyneuropathy	22.30	20.70	6	12286	217	50592615
Electrocardiogram QT prolonged	21.20	20.70	42	12250	51844	50540988
Alanine aminotransferase increased	21.18	20.70	58	12234	88301	50504531
General physical health deterioration	20.91	20.70	79	12213	142355	50450477
Basal cell carcinoma	20.81	20.70	27	12265	23329	50569503
Infective glossitis	20.74	20.70	4	12288	30	50592802

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	1252.96	19.30	1034	12602	286588	29274303
Malignant neoplasm progression	644.43	19.30	408	13228	73451	29487440
Chills	370.13	19.30	287	13349	71013	29489878
Metastases to central nervous system	355.62	19.30	131	13505	7000	29553891
Death	193.51	19.30	460	13176	341624	29219267
Ejection fraction decreased	192.43	19.30	109	13527	15869	29545022
Uveitis	134.22	19.30	62	13574	5885	29555006
Metastases to liver	89.32	19.30	60	13576	11796	29549095
Metastases to stomach	74.44	19.30	15	13621	69	29560822
Visual impairment	71.53	19.30	78	13558	29630	29531261
Second primary malignancy	65.55	19.30	40	13596	6665	29554226
Basal cell carcinoma	64.28	19.30	57	13579	16853	29544038
Squamous cell carcinoma	61.19	19.30	45	13591	10206	29550685
Blood creatine phosphokinase increased	60.91	19.30	84	13552	40560	29520331
Off label use	58.72	19.30	33	13603	300767	29260124
Rash	57.52	19.30	205	13431	189614	29371277
Metastases to lung	54.99	19.30	38	13598	7817	29553074
Metastatic malignant melanoma	54.07	19.30	23	13613	1792	29559099
Chorioretinopathy	52.56	19.30	21	13615	1395	29559496
Melanoma recurrent	51.66	19.30	12	13624	118	29560773
Metastases to peritoneum	51.12	19.30	21	13615	1499	29559392
Blood lactate dehydrogenase increased	50.75	19.30	53	13583	19156	29541735
Hyperpyrexia	48.75	19.30	23	13613	2287	29558604
C-reactive protein increased	48.46	19.30	79	13557	44184	29516707
Metastases to skin	48.34	19.30	14	13622	344	29560547
Malignant melanoma	46.30	19.30	33	13603	7128	29553763
Panniculitis	44.94	19.30	18	13618	1203	29559688
Erythema nodosum	42.07	19.30	16	13620	931	29559960
Serous retinal detachment	41.89	19.30	13	13623	407	29560484
Metastases to bone	38.88	19.30	34	13602	9864	29551027
Malignant mesenteric neoplasm	38.51	19.30	8	13628	44	29560847
Hyperkeratosis	38.50	19.30	22	13614	3247	29557644
Metastases to meninges	38.33	19.30	16	13620	1189	29559702
Product use in unapproved indication	35.44	19.30	104	13532	86771	29474120
Jejunal ulcer perforation	35.28	19.30	8	13628	70	29560821
Drug interaction	35.19	19.30	24	13612	197361	29363530
Metastases to lymph nodes	34.31	19.30	22	13614	3995	29556896
Procalcitonin increased	33.58	19.30	16	13620	1626	29559265
Fatigue	33.02	19.30	254	13382	316567	29244324
Drug ineffective	32.53	19.30	75	13561	363095	29197796
Metastasis	32.35	19.30	20	13616	3409	29557482
Gastrointestinal wall thickening	32.16	19.30	14	13622	1154	29559737
Haemophagocytic lymphohistiocytosis	31.42	19.30	31	13605	10473	29550418
Metastases to heart	30.68	19.30	8	13628	131	29560760
Brain neoplasm	30.64	19.30	18	13618	2798	29558093
Tissue infiltration	29.94	19.30	7	13629	71	29560820
Intestinal metastasis	29.42	19.30	8	13628	155	29560736
Omental necrosis	29.36	19.30	6	13630	30	29560861
Mesenteric neoplasm	29.04	19.30	6	13630	32	29560859
Eastern Cooperative Oncology Group performance status	28.88	19.30	6	13630	33	29560858
Ureteral disorder	28.63	19.30	8	13628	172	29560719
Toxicity to various agents	28.50	19.30	23	13613	173638	29387253
Decreased appetite	28.16	19.30	137	13499	145205	29415686
Disease progression	27.79	19.30	92	13544	81824	29479067
Vision blurred	24.53	19.30	56	13580	40120	29520771
Anxiety	24.09	19.30	5	13631	85360	29475531
Papilloedema	23.08	19.30	14	13622	2306	29558585
Nausea	21.77	19.30	216	13420	289039	29271852
Bacterial diarrhoea	21.63	19.30	5	13631	48	29560843
Vomiting	21.38	19.30	169	13467	212091	29348800
Tumour invasion	20.91	19.30	7	13629	280	29560611
Inflammatory bowel disease	20.59	19.30	13	13623	2298	29558593
Iridocyclitis	20.55	19.30	11	13625	1429	29559462
Body temperature fluctuation	20.48	19.30	11	13625	1439	29559452
Small intestine carcinoma	20.42	19.30	8	13628	504	29560387
Leukoderma	20.39	19.30	5	13631	63	29560828
Overdose	19.95	19.30	6	13630	79813	29481078
Dermatitis acneiform	19.85	19.30	18	13618	5473	29555418
Rectal polyp	19.48	19.30	8	13628	570	29560321

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	1955.22	18.07	1546	19976	557098	63920112
Malignant neoplasm progression	1028.47	18.07	572	20950	112299	64364911
Chills	513.41	18.07	399	21123	136865	64340345
Metastases to central nervous system	411.60	18.07	160	21362	13752	64463458
Uveitis	299.15	18.07	124	21398	12584	64464626
Ejection fraction decreased	292.16	18.07	157	21365	28550	64448660
Death	261.91	18.07	527	20995	482178	63995032
Panniculitis	129.59	18.07	62	21460	8817	64468393
Blood creatine phosphokinase increased	123.08	18.07	123	21399	58435	64418775
Squamous cell carcinoma	101.01	18.07	61	21461	13808	64463402
Erythema nodosum	93.95	18.07	39	21483	3965	64473245
Chorioretinopathy	93.39	18.07	33	21489	2164	64475046
Blood lactate dehydrogenase increased	91.60	18.07	81	21441	32997	64444213
Second primary malignancy	89.17	18.07	54	21468	12283	64464927
Drug ineffective	84.46	18.07	94	21428	840153	63637057
Rash	83.69	18.07	338	21184	458211	64018999
Serous retinal detachment	82.88	18.07	23	21499	675	64476535
Basal cell carcinoma	82.38	18.07	74	21448	30764	64446446
Hyperpyrexia	78.82	18.07	37	21485	5040	64472170
Metastases to liver	77.24	18.07	64	21458	23877	64453333
Dermatitis acneiform	74.33	18.07	42	21480	8401	64468809
Off label use	72.47	18.07	63	21459	632743	63844467
Malignant melanoma	71.89	18.07	48	21474	12916	64464294
C-reactive protein increased	71.71	18.07	120	21402	94789	64382421
Metastases to lung	67.07	18.07	49	21473	15215	64461995
Hyperkeratosis	66.40	18.07	36	21486	6645	64470565
Melanoma recurrent	66.37	18.07	15	21507	184	64477026
Metastatic malignant melanoma	63.86	18.07	26	21496	2515	64474695
Metastases to stomach	62.50	18.07	15	21507	243	64476967
Metastasis	60.28	18.07	32	21490	5663	64471547
Metastases to meninges	57.99	18.07	25	21497	2790	64474420
Iridocyclitis	56.10	18.07	25	21497	3020	64474190
BRAF V600E mutation positive	54.81	18.07	10	21512	36	64477174
Haemophagocytic lymphohistiocytosis	54.57	18.07	46	21476	17563	64459647
Rash maculo-papular	51.94	18.07	71	21451	46955	64430255
Visual impairment	51.12	18.07	90	21432	73987	64403223
Drug interaction	50.63	18.07	29	21493	362054	64115156
Cutaneous sarcoidosis	50.34	18.07	14	21508	414	64476796
Condition aggravated	49.06	18.07	32	21490	372394	64104816
Metastases to bone	48.67	18.07	46	21476	20389	64456821
Procalcitonin increased	47.66	18.07	21	21501	2470	64474740
Drug hypersensitivity	46.73	18.07	11	21511	237804	64239406
Skin toxicity	45.41	18.07	28	21494	6574	64470636
Metastases to lymph nodes	45.28	18.07	31	21491	8686	64468524
Vogt-Koyanagi-Harada disease	44.74	18.07	11	21511	198	64477012
Toxicity to various agents	44.23	18.07	34	21488	363479	64113731
Metastases to skin	43.97	18.07	17	21505	1435	64475775
Metastases to peritoneum	43.49	18.07	22	21500	3525	64473685
Decreased appetite	42.42	18.07	196	21326	281093	64196117
Product use in unapproved indication	41.09	18.07	141	21381	176477	64300733
Rheumatoid arthritis	40.41	18.07	4	21518	164290	64312920
Malignant mesenteric neoplasm	39.81	18.07	8	21514	53	64477157
Vomiting	38.83	18.07	315	21207	550802	63926408
Squamous cell carcinoma of skin	38.82	18.07	32	21490	11844	64465366
Dehydration	38.74	18.07	159	21363	216604	64260606
Aspartate aminotransferase increased	38.44	18.07	107	21415	119681	64357529
Retinal detachment	38.23	18.07	27	21495	7949	64469261
Jejunal ulcer perforation	34.55	18.07	8	21514	110	64477100
Demyelinating polyneuropathy	33.36	18.07	14	21508	1462	64475748
Vision blurred	33.34	18.07	85	21437	90231	64386979
Pneumonitis	33.21	18.07	60	21462	50305	64426905
Palmar-plantar erythrodysaesthesia syndrome	32.56	18.07	44	21478	28775	64448435
Keratoacanthoma	32.28	18.07	12	21510	910	64476300
Overdose	32.09	18.07	7	21515	159559	64317651
Detachment of retinal pigment epithelium	31.95	18.07	11	21511	667	64476543
Anxiety	31.64	18.07	14	21508	202635	64274575
Blood alkaline phosphatase increased	30.87	18.07	62	21460	56217	64420993
Eastern Cooperative Oncology Group performance status	30.23	18.07	6	21516	37	64477173
General physical health deterioration	29.72	18.07	141	21381	204284	64272926
Hypophysitis	29.44	18.07	17	21505	3542	64473668
Metastases to adrenals	29.31	18.07	12	21510	1177	64476033
Omental necrosis	29.21	18.07	6	21516	45	64477165
BRAF gene mutation	29.09	18.07	6	21516	46	64477164
Hepatocellular injury	28.70	18.07	53	21469	45182	64432028
Gastrointestinal wall thickening	28.60	18.07	14	21508	2091	64475119
Disease progression	28.58	18.07	108	21414	141572	64335638
Palmoplantar keratoderma	28.48	18.07	9	21513	417	64476793
Intestinal metastasis	28.13	18.07	8	21514	257	64476953
Nausea	27.83	18.07	391	21131	785409	63691801
Mesenteric neoplasm	27.67	18.07	6	21516	60	64477150
Autoimmune colitis	27.50	18.07	12	21510	1379	64475831
Hypersensitivity	27.05	18.07	16	21506	196436	64280774
Abdominal lymphadenopathy	26.52	18.07	11	21511	1115	64476095
Sinusitis	26.28	18.07	8	21514	145920	64331290
Gamma-glutamyltransferase increased	26.08	18.07	53	21469	48457	64428753
Tumour invasion	25.82	18.07	8	21514	347	64476863
Myalgia	25.72	18.07	113	21409	158504	64318706
Rhabdomyolysis	25.63	18.07	78	21444	91648	64385562
Concomitant disease aggravated	25.62	18.07	25	21497	11517	64465693
Alanine aminotransferase increased	25.62	18.07	103	21419	138928	64338282
Papilloedema	24.92	18.07	18	21504	5487	64471723
Metastases to heart	24.67	18.07	7	21515	223	64476987
Therapeutic product effect incomplete	24.22	18.07	3	21519	103479	64373731
Influenza like illness	23.74	18.07	59	21463	61643	64415567
Dyspnoea	23.62	18.07	142	21380	718532	63758678
Fatigue	23.52	18.07	365	21157	748365	63728845
Ureteral disorder	23.05	18.07	8	21514	497	64476713
Lipase increased	22.71	18.07	26	21496	14376	64462834
Body temperature fluctuation	22.71	18.07	14	21508	3284	64473926
Erysipelas	22.69	18.07	21	21501	9060	64468150
Product dose omission issue	22.67	18.07	19	21503	194728	64282482
Fall	22.55	18.07	68	21454	416758	64060452
Erythema multiforme	22.52	18.07	27	21495	15674	64461536
Blood pressure increased	22.44	18.07	15	21507	172537	64304673
Intentional product use issue	21.76	18.07	3	21519	95361	64381849
Weight increased	21.15	18.07	24	21498	213324	64263886
Insomnia	21.01	18.07	21	21501	197815	64279395
Joint swelling	20.52	18.07	25	21497	215357	64261853
Paronychia	20.20	18.07	17	21505	6475	64470735
Musculoskeletal stiffness	20.04	18.07	8	21514	123198	64354012
Small intestine carcinoma	19.39	18.07	8	21514	800	64476410
Left ventricular dysfunction	19.32	18.07	26	21496	16928	64460282
Bacterial diarrhoea	18.86	18.07	5	21517	123	64477087
Immunisation reaction	18.36	18.07	4	21518	41	64477169
Disseminated intravascular coagulation	18.17	18.07	36	21486	32312	64444898
Leukoderma	18.17	18.07	5	21517	142	64477068
Tissue infiltration	18.16	18.07	7	21515	586	64476624

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 (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 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 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	Oct. 6, 2022	ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 75MG BASE	TAFINLAR	NOVARTIS	N202806	May 29, 2013	RX	CAPSULE	ORAL	Oct. 6, 2022	ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
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	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

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
GTPase KRas	Enzyme	P01116	RASK_HUMAN		IC50	5.23	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
Serine/threonine-protein kinase Nek1	Kinase	Q96PY6	NEK1_HUMAN		Kd	6.32	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
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		IC50	8.70	CHEMBL
Serine/threonine-protein kinase A-Raf	Kinase	P10398	ARAF_HUMAN		IC50	7.59	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
CHEMBL523411	ChEMBL_ID
C561627	MESH_SUPPLEMENTAL_RECORD_UI
6494	IUPHAR_LIGAND_ID
9458	INN_ID
DB08912	DRUGBANK_ID
QGP4HA4G1B	UNII
44462760	PUBCHEM_CID
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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	32 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0681	CAPSULE	75 mg	ORAL	NDA	32 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	32 sections
Tafinlar	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0682	CAPSULE	50 mg	ORAL	NDA	32 sections