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

Stem definitionDrug idCAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors 4801 1195765-45-7

Description:

MoleculeDescription

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:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pyrexia 1347.94 19.84 969 12663 417804 55860631
Malignant neoplasm progression 750.30 19.84 362 13270 73225 56205210
Chills 374.99 19.84 259 13373 102345 56176090
Metastatic malignant melanoma 368.98 19.84 83 13549 1407 56277028
Uveitis 243.16 19.84 94 13538 11001 56267434
Death 237.44 19.84 348 13284 341078 55937357
Malignant melanoma 235.57 19.84 91 13541 10628 56267807
Metastases to central nervous system 231.51 19.84 93 13539 12043 56266392
Panniculitis 126.44 19.84 57 13575 9785 56268650
Visual impairment 118.66 19.84 116 13516 74086 56204349
Malignant melanoma stage IV 114.18 19.84 19 13613 52 56278383
Ejection fraction decreased 104.06 19.84 63 13569 19778 56258657
Drug ineffective 79.72 19.84 64 13568 918925 55359510
Erythema nodosum 75.52 19.84 31 13601 4234 56274201
Rash 73.89 19.84 274 13358 492773 55785662
Blood creatine phosphokinase increased 73.46 19.84 58 13574 27894 56250541
Dermatitis acneiform 64.96 19.84 28 13604 4316 56274119
Anaplastic thyroid cancer 58.01 19.84 10 13622 36 56278399
Serous retinal detachment 55.36 19.84 13 13619 268 56278167
Vision blurred 54.99 19.84 83 13549 82860 56195575
Product use in unapproved indication 54.32 19.84 111 13521 140711 56137724
Second primary malignancy 50.78 19.84 28 13604 7374 56271061
Chorioretinopathy 49.83 19.84 15 13617 819 56277616
Skin toxicity 46.90 19.84 22 13610 4131 56274304
Vogt-Koyanagi-Harada disease 46.49 19.84 10 13622 136 56278299
Drug hypersensitivity 46.34 19.84 6 13626 275199 56003236
Hyperpyrexia 45.40 19.84 20 13612 3248 56275187
Nausea 44.97 19.84 327 13305 763851 55514584
Iridocyclitis 41.90 19.84 17 13615 2252 56276183
Off label use 41.77 19.84 44 13588 556136 55722299
Metastasis 41.02 19.84 21 13611 4763 56273672
Vomiting 40.80 19.84 232 13400 497996 55780439
Rash maculo-papular 40.30 19.84 42 13590 28865 56249570
Non-small cell lung cancer 40.15 19.84 19 13613 3639 56274796
Blood lactate dehydrogenase increased 40.06 19.84 36 13596 20639 56257796
BRAF V600E mutation positive 39.64 19.84 7 13625 30 56278405
Erythema multiforme 39.24 19.84 26 13606 9528 56268907
Metastases to lung 38.96 19.84 28 13604 11690 56266745
Metastases to meninges 38.49 19.84 16 13616 2254 56276181
Melanoma recurrent 38.35 19.84 8 13624 93 56278342
Cutaneous sarcoidosis 37.01 19.84 10 13622 369 56278066
Ganglioglioma 36.74 19.84 6 13626 14 56278421
Condition aggravated 36.54 19.84 19 13613 344879 55933556
Hyperkeratosis 36.05 19.84 20 13612 5327 56273108
Palmar-plantar erythrodysaesthesia syndrome 33.74 19.84 33 13599 21032 56257403
Rhabdomyolysis 33.27 19.84 45 13587 40613 56237822
Dehydration 33.20 19.84 99 13533 158726 56119709
Sinusitis 31.62 19.84 5 13627 197576 56080859
Aspartate aminotransferase increased 30.51 19.84 64 13568 82538 56195897
Haemophagocytic lymphohistiocytosis 29.84 19.84 22 13610 9550 56268885
Abdominal discomfort 29.76 19.84 15 13617 277259 56001176
Systemic inflammatory response syndrome 28.28 19.84 17 13615 5261 56273174
Non-small cell lung cancer recurrent 27.93 19.84 6 13626 81 56278354
Retinal detachment 27.80 19.84 17 13615 5424 56273011
Pneumonitis 27.46 19.84 36 13596 31528 56246907
Vitreous floaters 27.44 19.84 17 13615 5550 56272885
Myalgia 27.30 19.84 82 13550 131943 56146492
Arthropathy 26.14 19.84 8 13624 200267 56078168
Squamous cell carcinoma 26.02 19.84 19 13613 8129 56270306
Panniculitis lobular 26.00 19.84 5 13627 37 56278398
Paronychia 24.20 19.84 15 13617 4903 56273532
Discomfort 24.05 19.84 3 13629 141758 56136677
Decreased appetite 23.34 19.84 110 13522 219121 56059314
Alanine aminotransferase increased 23.08 19.84 62 13570 93600 56184835
Leukoderma 22.31 19.84 5 13627 83 56278352
Acute polyneuropathy 22.24 19.84 6 13626 220 56278215
Keratoacanthoma 22.22 19.84 7 13625 445 56277990
Electrocardiogram QT prolonged 22.17 19.84 44 13588 54544 56223891
Treatment failure 21.89 19.84 7 13625 170385 56108050
Hypersensitivity 21.88 19.84 18 13614 256390 56022045
Fall 21.85 19.84 33 13599 357477 55920958
Dry skin 21.62 19.84 40 13592 47069 56231366
Joint swelling 21.60 19.84 23 13609 289777 55988658
Astrocytoma 21.58 19.84 5 13627 97 56278338
C-reactive protein increased 21.35 19.84 54 13578 78630 56199805
Infective glossitis 20.75 19.84 4 13628 30 56278405
Blood alkaline phosphatase increased 20.35 19.84 35 13597 38910 56239525
General physical health deterioration 20.10 19.84 88 13544 169922 56108513

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pyrexia 1305.87 19.08 1093 13800 302747 31379704
Malignant neoplasm progression 673.17 19.08 433 14460 78565 31603886
Metastatic malignant melanoma 485.03 19.08 128 14765 2167 31680284
Chills 391.84 19.08 304 14589 73846 31608605
Metastases to central nervous system 373.52 19.08 139 14754 7497 31674954
Malignant melanoma 272.93 19.08 111 14782 7596 31674855
Death 205.51 19.08 492 14401 360077 31322374
Ejection fraction decreased 184.25 19.08 110 14783 17324 31665127
Uveitis 134.01 19.08 65 14828 6751 31675700
Metastases to liver 93.81 19.08 64 14829 12663 31669788
Malignant melanoma stage IV 83.74 19.08 16 14877 51 31682400
Visual impairment 82.59 19.08 87 14806 31192 31651259
Second primary malignancy 75.88 19.08 45 14848 6987 31675464
Metastases to stomach 74.15 19.08 15 14878 69 31682382
Basal cell carcinoma 69.53 19.08 62 14831 18117 31664334
Off label use 67.45 19.08 40 14853 347234 31335217
Metastases to lung 61.22 19.08 42 14851 8380 31674071
Squamous cell carcinoma 60.87 19.08 46 14847 10665 31671786
Rash 59.87 19.08 219 14674 201267 31481184
Blood creatine phosphokinase increased 59.05 19.08 85 14808 41889 31640562
Melanoma recurrent 56.08 19.08 13 14880 124 31682327
Anaplastic thyroid cancer 52.79 19.08 9 14884 11 31682440
Chorioretinopathy 51.84 19.08 21 14872 1418 31681033
Hyperpyrexia 50.53 19.08 24 14869 2377 31680074
Blood lactate dehydrogenase increased 49.14 19.08 54 14839 20285 31662166
Metastases to peritoneum 48.95 19.08 21 14872 1639 31680812
Product use in unapproved indication 48.17 19.08 128 14765 99043 31583408
C-reactive protein increased 45.72 19.08 82 14811 48568 31633883
Metastases to skin 45.42 19.08 14 14879 420 31682031
Panniculitis 44.17 19.08 20 14873 1776 31680675
Hyperkeratosis 42.51 19.08 24 14869 3396 31679055
Serous retinal detachment 42.38 19.08 14 14879 527 31681924
Drug interaction 40.41 19.08 24 14869 208519 31473932
Metastases to meninges 40.18 19.08 17 14876 1282 31681169
Haemophagocytic lymphohistiocytosis 39.14 19.08 37 14856 11641 31670810
Erythema nodosum 38.85 19.08 16 14877 1127 31681324
Malignant mesenteric neoplasm 38.36 19.08 8 14885 44 31682407
Fatigue 36.24 19.08 275 14618 334931 31347520
Metastases to bone 35.65 19.08 34 14859 10814 31671637
Metastases to lymph nodes 35.13 19.08 23 14870 4245 31678206
Jejunal ulcer perforation 35.13 19.08 8 14885 70 31682381
Vision blurred 33.58 19.08 66 14827 41849 31640602
Metastasis 33.47 19.08 21 14872 3603 31678848
Procalcitonin increased 33.01 19.08 16 14877 1657 31680794
Drug ineffective 31.64 19.08 89 14804 395484 31286967
Toxicity to various agents 30.97 19.08 24 14869 181463 31500988
Metastases to heart 30.20 19.08 8 14885 137 31682314
Tissue infiltration 29.72 19.08 7 14886 72 31682379
Gastrointestinal wall thickening 29.46 19.08 14 14879 1388 31681063
Brain neoplasm 29.27 19.08 18 14875 2982 31679469
Omental necrosis 29.25 19.08 6 14887 30 31682421
Intestinal metastasis 29.08 19.08 8 14885 159 31682292
Mesenteric neoplasm 28.92 19.08 6 14887 32 31682419
Eastern Cooperative Oncology Group performance status 28.77 19.08 6 14887 33 31682418
Decreased appetite 28.70 19.08 145 14748 153072 31529379
Ureteral disorder 28.44 19.08 8 14885 173 31682278
Disease progression 25.64 19.08 97 14796 90367 31592084
Nausea 25.43 19.08 238 14655 307709 31374742
Anxiety 25.03 19.08 6 14887 91027 31591424
Papilloedema 24.25 19.08 15 14878 2511 31679940
Retinal detachment 23.12 19.08 19 14874 4967 31677484
Vomiting 22.59 19.08 181 14712 223792 31458659
Overdose 22.47 19.08 6 14887 84658 31597793
Iridocyclitis 22.43 19.08 12 14881 1528 31680923
Malignant melanoma stage III 21.94 19.08 4 14889 9 31682442
General physical health deterioration 21.67 19.08 108 14785 113327 31569124
Metastases to adrenals 21.59 19.08 10 14883 935 31681516
Depression 21.32 19.08 8 14885 90807 31591644
BRAF gene mutation 21.26 19.08 5 14888 51 31682400
Bacterial diarrhoea 21.00 19.08 5 14888 54 31682397
Tumour invasion 20.59 19.08 7 14886 288 31682163
Lung adenocarcinoma stage IV 20.21 19.08 6 14887 158 31682293
Leukoderma 20.08 19.08 5 14888 66 31682385
Abdominal lymphadenopathy 19.95 19.08 9 14884 792 31681659
Liver function test increased 19.72 19.08 27 14866 12687 31669764
Febrile neutropenia 19.66 19.08 17 14876 121832 31560619
BRAF V600E mutation positive 19.33 19.08 4 14889 21 31682430
Body temperature fluctuation 19.25 19.08 11 14882 1592 31680859
Inflammatory bowel disease 19.23 19.08 13 14880 2530 31679921

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pyrexia 1990.47 17.66 1604 21583 605348 70299909
Malignant neoplasm progression 1096.47 17.66 608 22579 121131 70784126
Metastatic malignant melanoma 613.03 17.66 153 23034 3011 70902246
Chills 523.20 17.66 409 22778 144377 70760880
Metastases to central nervous system 430.82 17.66 168 23019 14866 70890391
Malignant melanoma 379.53 17.66 150 23037 13750 70891507
Uveitis 302.63 17.66 130 23057 14715 70890542
Death 299.69 17.66 569 22618 509492 70395765
Ejection fraction decreased 293.26 17.66 160 23027 30602 70874655
Malignant melanoma stage IV 199.13 17.66 37 23150 155 70905102
Blood creatine phosphokinase increased 126.01 17.66 126 23061 61137 70844120
Panniculitis 125.74 17.66 64 23123 10612 70894645
Squamous cell carcinoma 101.81 17.66 62 23125 14542 70890715
Second primary malignancy 100.31 17.66 59 23128 12992 70892265
Erythema nodosum 97.10 17.66 41 23146 4440 70900817
Blood lactate dehydrogenase increased 96.75 17.66 85 23102 35042 70870215
Chorioretinopathy 93.64 17.66 33 23154 2192 70903065
Off label use 92.91 17.66 65 23122 742995 70162262
Basal cell carcinoma 87.75 17.66 79 23108 33619 70871638
Drug ineffective 87.17 17.66 108 23079 939644 69965613
Serous retinal detachment 87.15 17.66 25 23162 847 70904410
Hyperpyrexia 86.80 17.66 40 23147 5334 70899923
Anaplastic thyroid cancer 82.31 17.66 15 23172 55 70905202
Metastases to lung 80.54 17.66 56 23131 16428 70888829
Metastases to liver 80.18 17.66 67 23120 25811 70879446
Rheumatoid arthritis 78.89 17.66 4 23183 291801 70613456
Rash 77.56 17.66 351 22836 510211 70395046
Haemophagocytic lymphohistiocytosis 74.01 17.66 57 23130 19555 70885702
Dermatitis acneiform 72.87 17.66 42 23145 8903 70896354
Melanoma recurrent 71.45 17.66 16 23171 192 70905065
Hyperkeratosis 67.88 17.66 37 23150 7047 70898210
Metastasis 67.22 17.66 35 23152 6079 70899178
C-reactive protein increased 66.45 17.66 125 23062 110392 70794865
Metastases to stomach 62.80 17.66 15 23172 243 70905014
BRAF V600E mutation positive 61.10 17.66 11 23176 37 70905220
Iridocyclitis 60.76 17.66 27 23160 3308 70901949
Metastases to meninges 59.10 17.66 26 23161 3110 70902147
Ganglioglioma 57.19 17.66 10 23177 27 70905230
Condition aggravated 56.57 17.66 35 23152 427600 70477657
Drug hypersensitivity 52.33 17.66 11 23176 262448 70642809
Visual impairment 52.30 17.66 94 23093 80156 70825101
Drug interaction 52.15 17.66 30 23157 381411 70523846
Rash maculo-papular 52.05 17.66 73 23114 50472 70854785
Skin toxicity 51.30 17.66 31 23156 7167 70898090
Procalcitonin increased 50.31 17.66 22 23165 2594 70902663
Cutaneous sarcoidosis 48.70 17.66 14 23173 478 70904779
Metastases to lymph nodes 46.57 17.66 32 23155 9206 70896051
Metastases to bone 45.93 17.66 46 23141 22330 70882927
Metastases to peritoneum 45.27 17.66 23 23164 3796 70901461
Retinal detachment 44.28 17.66 30 23157 8437 70896820
Decreased appetite 44.25 17.66 207 22980 304573 70600684
Vogt-Koyanagi-Harada disease 43.73 17.66 11 23176 223 70905034
Metastases to skin 43.01 17.66 17 23170 1554 70903703
Product use in unapproved indication 42.77 17.66 157 23030 207321 70697936
Toxicity to various agents 41.87 17.66 38 23149 382134 70523123
Vision blurred 41.26 17.66 94 23093 94890 70810367
Aspartate aminotransferase increased 40.79 17.66 112 23075 126866 70778391
Malignant mesenteric neoplasm 39.98 17.66 8 23179 53 70905204
Vomiting 39.25 17.66 329 22858 592782 70312475
Dehydration 39.19 17.66 162 23025 225980 70679277
BRAF gene mutation 39.11 17.66 8 23179 60 70905197
Detachment of retinal pigment epithelium 38.97 17.66 13 23174 731 70904526
Squamous cell carcinoma of skin 37.49 17.66 32 23155 12680 70892577
Demyelinating polyneuropathy 35.90 17.66 15 23172 1582 70903675
Malignant melanoma stage III 35.87 17.66 7 23180 40 70905217
Blood alkaline phosphatase increased 34.91 17.66 66 23121 58455 70846802
Jejunal ulcer perforation 34.72 17.66 8 23179 110 70905147
Non-small cell lung cancer 34.41 17.66 23 23164 6324 70898933
Overdose 34.05 17.66 7 23180 169738 70735519
Anxiety 33.56 17.66 15 23172 220315 70684942
Palmar-plantar erythrodysaesthesia syndrome 33.11 17.66 45 23142 30202 70875055
Pneumonitis 33.10 17.66 62 23125 54535 70850722
Metastases to adrenals 32.47 17.66 13 23174 1229 70904028
Intestinal metastasis 31.98 17.66 9 23178 284 70904973
Keratoacanthoma 31.93 17.66 12 23175 957 70904300
Sinusitis 31.89 17.66 8 23179 169187 70736070
Hypophysitis 31.56 17.66 18 23169 3740 70901517
Anaplastic astrocytoma 31.27 17.66 8 23179 174 70905083
Hypersensitivity 30.08 17.66 19 23168 229793 70675464
Eastern Cooperative Oncology Group performance status 29.57 17.66 6 23181 43 70905214
Omental necrosis 29.33 17.66 6 23181 45 70905212
General physical health deterioration 29.02 17.66 153 23034 235878 70669379
Abdominal lymphadenopathy 28.93 17.66 12 23175 1242 70904015
Gamma-glutamyltransferase increased 28.80 17.66 56 23131 50629 70854628
Hepatocellular injury 28.76 17.66 53 23134 46038 70859219
Nausea 28.60 17.66 413 22774 851675 70053582
Intentional product use issue 28.59 17.66 3 23184 120139 70785118
Therapeutic product effect incomplete 28.51 17.66 3 23184 119879 70785378
Palmoplantar keratoderma 28.19 17.66 9 23178 440 70904817
Mesenteric neoplasm 27.27 17.66 6 23181 66 70905191
Gastrointestinal wall thickening 27.27 17.66 14 23173 2362 70902895
Disease progression 26.93 17.66 112 23075 156560 70748697
Concomitant disease aggravated 26.90 17.66 26 23161 12088 70893169
Joint swelling 26.74 17.66 26 23161 253185 70652072
Weight increased 26.63 17.66 24 23163 242307 70662950
Autoimmune colitis 26.61 17.66 12 23175 1522 70903735
Alanine aminotransferase increased 26.59 17.66 107 23080 147373 70757884
Papilloedema 26.46 17.66 19 23168 5859 70899398
Rhabdomyolysis 26.42 17.66 80 23107 95680 70809577
Musculoskeletal stiffness 25.95 17.66 8 23179 147752 70757505
Product dose omission issue 25.78 17.66 20 23167 217448 70687809
Tumour invasion 25.68 17.66 8 23179 361 70904896
Blood pressure increased 25.48 17.66 15 23172 188502 70716755
Paronychia 25.47 17.66 20 23167 7054 70898203
Lipase increased 25.32 17.66 28 23159 15218 70890039
Non-small cell lung cancer recurrent 25.02 17.66 6 23181 99 70905158
Dyspnoea 24.83 17.66 149 23038 769911 70135346
Fall 24.24 17.66 70 23117 444026 70461231
Metastases to heart 23.65 17.66 7 23180 265 70904992
Myalgia 23.56 17.66 113 23074 167779 70737478
Astrocytoma 23.50 17.66 7 23180 271 70904986
Arthropathy 23.18 17.66 10 23177 150047 70755210
Ureteral disorder 22.97 17.66 8 23179 513 70904744
Influenza like illness 22.34 17.66 59 23128 65272 70839985
Insomnia 22.26 17.66 23 23164 217783 70687474
Intentional overdose 22.08 17.66 3 23184 98432 70806825
Psoriasis 22.08 17.66 3 23184 98430 70806827
Body temperature fluctuation 21.99 17.66 14 23173 3545 70901712
Erythema multiforme 21.81 17.66 27 23160 16537 70888720
Fatigue 21.76 17.66 384 22803 823935 70081322
Abdominal discomfort 21.57 17.66 23 23164 214635 70690622
Erysipelas 21.47 17.66 21 23166 9903 70895354
Lung adenocarcinoma stage IV 21.31 17.66 7 23180 375 70904882
Vitiligo 21.27 17.66 11 23176 1884 70903373
Disseminated intravascular coagulation 20.17 17.66 38 23149 33560 70871697
Treatment failure 20.15 17.66 11 23176 144131 70761126
Left ventricular dysfunction 20.08 17.66 27 23160 17930 70887327
Nasopharyngitis 19.98 17.66 26 23161 222180 70683077
Asthenia 19.54 17.66 232 22955 457434 70447823
Amylase increased 19.16 17.66 20 23167 10188 70895069
Therapy cessation 18.88 17.66 37 23150 33639 70871618
Brain oedema 18.64 17.66 30 23157 23388 70881869
Metastatic neoplasm 18.61 17.66 14 23173 4634 70900623
Peripheral motor neuropathy 18.56 17.66 12 23175 3120 70902137
Visual acuity reduced 18.54 17.66 33 23154 27897 70877360
Sarcoidosis 18.16 17.66 16 23171 6611 70898646
Small intestine carcinoma 18.06 17.66 8 23179 972 70904285
Swelling 18.06 17.66 21 23166 188518 70716739
Vitreous floaters 18.00 17.66 16 23171 6688 70898569
Panniculitis lobular 17.94 17.66 4 23183 47 70905210
Leukoderma 17.85 17.66 5 23182 155 70905102
Cerebral haemorrhage 17.76 17.66 48 23139 53816 70851441

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.56 acidic
pKa2 3.35 Basic
pKa3 0.43 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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
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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Serine/threonine-protein kinase B-raf Kinase INHIBITOR IC50 9.16 WOMBAT-PK CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.11 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.89 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 6.09 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase IC50 6.82 CHEMBL
Cyclin-dependent kinase 1 Kinase Kd 6.44 CHEMBL
Cyclin-dependent kinase 2 Kinase Kd 7.72 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.78 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 5.49 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 6.07 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.79 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.87 CHEMBL
LIM domain kinase 1 Kinase Kd 7.48 CHEMBL
Cyclin-dependent-like kinase 5 Kinase Kd 5.97 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 6.28 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.52 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.81 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.14 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase IC50 7.11 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 7.89 CHEMBL
Activin receptor type-1B Kinase Kd 6.22 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.60 CHEMBL
Cyclin-dependent kinase 6 Kinase Kd 6.50 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 5.85 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 7.18 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 7.44 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 6.74 CHEMBL
LIM domain kinase 2 Kinase Kd 7.09 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 5.74 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 6.19 CHEMBL
Calcium/calmodulin-dependent protein kinase type IV Kinase Kd 5.64 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 6 CHEMBL
Serine/threonine-protein kinase Nek9 Kinase Kd 7.28 CHEMBL
TGF-beta receptor type-1 Kinase IC50 5.43 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 6.15 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 7.47 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 6.92 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase IC50 4.27 CHEMBL
Cyclin-dependent kinase 4 Kinase Kd 6.90 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.38 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 5.84 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 5.81 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 6.73 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.83 CHEMBL
Serine/threonine-protein kinase SIK3 Kinase Kd 5.70 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1 Kinase Kd 6.02 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 5.64 CHEMBL
Dual serine/threonine and tyrosine protein kinase Kinase IC50 4.53 CHEMBL
Serine/threonine-protein kinase A-Raf Kinase IC50 7.59 CHEMBL
GTPase KRas Enzyme IC50 5.23 CHEMBL
Serine/threonine-protein kinase Nek1 Kinase Kd 6.32 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase IC50 8.70 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 5.81 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE2 Kinase Kd 6.94 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 0078-0681 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
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-0682 CAPSULE 50 mg ORAL NDA 32 sections