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 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 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 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 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 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:

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 (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

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 ABL1 Kinase Kd 5.81 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
GTPase KRas Enzyme IC50 5.23 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
Serine/threonine-protein kinase Nek1 Kinase Kd 6.32 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
Receptor-interacting serine/threonine-protein kinase 3 Kinase IC50 8.70 CHEMBL
Serine/threonine-protein kinase A-Raf Kinase IC50 7.59 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
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:

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