dabrafenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.930 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.837 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 71.285 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 8.279 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 1.190 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 2.630 % High 1
herg hERG pIC50 4.784 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 15.812 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 40.365 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.790 % High 1
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK7,CDK9,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,IRAK1,ITK,JAK1,JAK2,KDR,KIT,LYN,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK7,MAPK9,MARK4,MELK,MET,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,TYRO3,UHMK1,ULK1,ULK2 75
kinase-selectivity-class ACVR2B,AURKA,AXL,BRAF,CDK1,CDK9,DDR1,DYRK1B,EGFR,ERBB2,GRK2,MAP2K6,MAP3K10,MAP3K21,MAP4K1,MAPK7,PDK1,PIK3CA,PIK3CB,PIK3CD,PRKCD,PRKDC,SIK2,SIK3,TEK,ULK1 26
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.624 High 1
mh-clint Mouse hepatocyte intrinsic clearance 49.774 High 1
mppb Mouse plasma protein binding (% unbound) 1.150 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 23.823 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 2.020 % High 1
rh-clint Rat hepatocyte intrinsic clearance 53.580 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 22.500 % High 1
rppb Rat plasma protein binding (% unbound) 0.720 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 8.551 uM High 1

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 1738.09 21.57 1267 17296 659218 89950666
Malignant neoplasm progression 1120.88 21.57 509 18054 106361 90503523
Chills 545.44 21.57 338 18225 131643 90478241
Death 397.75 21.57 477 18086 456074 90153810
Metastases to central nervous system 308.50 21.57 121 18442 17421 90592463
Uveitis 305.61 21.57 117 18446 15786 90594098
Visual impairment 243.81 21.57 208 18355 132157 90477727
Panniculitis 200.13 21.57 84 18479 14374 90595510
Ejection fraction decreased 146.95 21.57 82 18481 26171 90583713
Vision blurred 129.28 21.57 135 18428 110158 90499726
Rash 120.81 21.57 397 18166 795703 89814181
Blood creatine phosphokinase increased 119.92 21.57 79 18484 33944 90575940
Erythema nodosum 116.73 21.57 44 18519 5680 90604204
Skin toxicity 112.97 21.57 45 18518 6734 90603150
Metastatic malignant melanoma 100.93 21.57 29 18534 1595 90608289
Nausea 90.09 21.57 456 18107 1109860 89500024
Serous retinal detachment 85.94 21.57 21 18542 613 90609271
Dermatitis acneiform 81.55 21.57 35 18528 6319 90603565
Drug ineffective 80.24 21.57 100 18463 1384198 89225686
Hyperpyrexia 77.23 21.57 31 18532 4730 90605154
Iridocyclitis 74.13 21.57 28 18535 3633 90606251
Metastases to lung 71.03 21.57 43 18520 15948 90593936
Vogt-Koyanagi-Harada disease 67.93 21.57 16 18547 398 90609486
BRAF V600E mutation positive 64.74 21.57 11 18552 44 90609840
Squamous cell carcinoma 63.27 21.57 34 18529 10067 90599817
Drug hypersensitivity 62.65 21.57 10 18553 463599 90146285
Rheumatoid arthritis 61.78 21.57 3 18560 362611 90247273
Vomiting 61.04 21.57 320 18243 787973 89821911
Hyperkeratosis 59.94 21.57 29 18534 6899 90602985
Product use in unapproved indication 56.44 21.57 174 18389 336062 90273822
Malignant melanoma 56.33 21.57 34 18529 12542 90597342
Chorioretinopathy 55.96 21.57 16 18547 864 90609020
Condition aggravated 53.02 21.57 28 18535 595517 90014367
Second primary malignancy 51.56 21.57 30 18533 10348 90599536
Arthropathy 51.54 21.57 7 18556 366235 90243649
Metastasis 51.03 21.57 25 18538 6112 90603772
Melanoma recurrent 50.62 21.57 11 18552 188 90609696
Myalgia 50.41 21.57 111 18452 175014 90434870
Maternal exposure during pregnancy 50.39 21.57 7 18556 360056 90249828
Palmar-plantar erythrodysaesthesia syndrome 49.37 21.57 43 18520 27980 90581904
Fatigue 49.14 21.57 403 18160 1153620 89456264
Off label use 49.00 21.57 95 18468 1102157 89507727
Wound 47.18 21.57 4 18559 302976 90306908
Rash maculo-papular 45.94 21.57 49 18514 40884 90569000
Retinal detachment 45.66 21.57 24 18539 6798 90603086
Dehydration 44.81 21.57 113 18450 194334 90415550
Erythema multiforme 44.51 21.57 29 18534 12217 90597667
Sinusitis 42.88 21.57 9 18554 343079 90266805
Rhabdomyolysis 41.75 21.57 52 18511 51204 90558680
Hyperthermia 41.34 21.57 26 18537 10309 90599575
Blood lactate dehydrogenase increased 40.16 21.57 37 18526 25895 90583989
Metastases to meninges 39.62 21.57 18 18545 3717 90606167
Sarcoid-like reaction 39.48 21.57 9 18554 193 90609691
Aspartate aminotransferase increased 38.82 21.57 73 18490 102864 90507020
Metastases to lymph nodes 38.42 21.57 26 18537 11663 90598221
Haemophagocytic lymphohistiocytosis 38.41 21.57 29 18534 15430 90594454
Vitreous floaters 37.97 21.57 22 18541 7527 90602357
Treatment failure 37.92 21.57 8 18555 303920 90305964
Cutaneous sarcoidosis 36.64 21.57 10 18553 455 90609429
Diarrhoea 35.66 21.57 320 18243 938870 89671014
Systemic inflammatory response syndrome 35.49 21.57 20 18543 6496 90603388
Helicobacter infection 35.30 21.57 3 18560 226847 90383037
Wheezing 34.82 21.57 4 18559 238076 90371808
Discomfort 34.68 21.57 7 18556 274328 90335556
Weight increased 33.82 21.57 22 18541 417905 90191979
Pneumonitis 33.11 21.57 43 18520 44127 90565757
Musculoskeletal stiffness 32.77 21.57 10 18553 296522 90313362
Dysphagia 32.10 21.57 71 18492 112207 90497677
Disease progression 31.96 21.57 87 18476 156528 90453356
Non-small cell lung cancer recurrent 31.92 21.57 7 18556 125 90609759
Decreased appetite 31.18 21.57 156 18407 376384 90233500
Mobility decreased 28.53 21.57 8 18555 250726 90359158
Folliculitis 28.50 21.57 4 18559 204349 90405535
Joint swelling 28.29 21.57 37 18526 503263 90106621
Metastases to bone 27.68 21.57 30 18533 25475 90584409
Alanine aminotransferase increased 27.48 21.57 69 18494 118269 90491615
Asthenia 27.37 21.57 195 18368 533556 90076328
Nasopharyngitis 27.17 21.57 26 18537 407078 90202806
Hypersensitivity 27.05 21.57 32 18531 454645 90155239
Pulmonary embolism 27.02 21.57 73 18490 130747 90479137
Metastatic neoplasm 26.82 21.57 15 18548 4800 90605084
Cholestasis 26.68 21.57 35 18528 36264 90573620
Dry skin 26.66 21.57 57 18506 88016 90521868
Macular oedema 26.55 21.57 15 18548 4894 90604990
Type 2 diabetes mellitus 26.07 21.57 5 18558 203239 90406645
Gamma-glutamyltransferase increased 25.46 21.57 35 18528 37917 90571967
Panniculitis lobular 25.14 21.57 5 18558 54 90609830
Tumour haemorrhage 25.12 21.57 11 18552 2083 90607801
Neutrophilic panniculitis 24.89 21.57 5 18558 57 90609827
Blood cholesterol increased 24.88 21.57 6 18557 208006 90401878
Erysipelas 24.78 21.57 18 18545 9034 90600850
Disseminated intravascular coagulation 24.55 21.57 26 18537 21512 90588372
Intentional product use issue 24.53 21.57 7 18556 216885 90392999
Transaminases increased 24.50 21.57 34 18529 37158 90572726
Paronychia 24.40 21.57 17 18546 7989 90601895
Acute polyneuropathy 23.24 21.57 7 18556 454 90609430
Electrocardiogram QT prolonged 23.21 21.57 48 18515 72408 90537476
Blood alkaline phosphatase increased 23.18 21.57 38 18525 48041 90561843
Hepatotoxicity 23.15 21.57 37 18526 45805 90564079
Metastases to liver 23.09 21.57 29 18534 28778 90581106
Fall 22.66 21.57 40 18523 481770 90128114
Leukoderma 22.61 21.57 5 18558 93 90609791
Insomnia 22.60 21.57 21 18542 333453 90276431
Swelling 22.34 21.57 32 18531 419026 90190858
Lymphadenopathy 21.83 21.57 36 18527 45739 90564145
Acrochordon 21.77 21.57 9 18554 1480 90608404
Brain oedema 21.63 21.57 22 18541 17363 90592521

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 1671.62 18.77 1384 17867 392658 42209426
Malignant neoplasm progression 910.13 18.77 580 18671 107820 42494264
Chills 556.35 18.77 406 18845 93660 42508424
Metastases to central nervous system 489.86 18.77 182 19069 10173 42591911
Death 290.20 18.77 647 18604 470538 42131546
Ejection fraction decreased 206.42 18.77 127 19124 21960 42580124
Visual impairment 194.86 18.77 159 19092 42954 42559130
Uveitis 181.42 18.77 87 19164 9171 42592913
Metastases to liver 104.14 18.77 74 19177 16252 42585832
Second primary malignancy 99.58 18.77 59 19192 9516 42592568
Blood creatine phosphokinase increased 89.91 18.77 110 19141 48228 42553856
Rash 84.80 18.77 296 18955 276658 42325426
Metastases to lung 78.02 18.77 54 19197 11370 42590714
Fatigue 75.25 18.77 391 18860 435250 42166834
Melanoma recurrent 73.55 18.77 17 19234 167 42601917
Serous retinal detachment 73.17 18.77 24 19227 920 42601164
Metastases to stomach 73.06 18.77 15 19236 79 42602005
Metastatic malignant melanoma 67.73 18.77 29 19222 2344 42599740
Basal cell carcinoma 67.15 18.77 66 19185 22667 42579417
Squamous cell carcinoma 65.23 18.77 51 19200 12931 42589153
Off label use 61.26 18.77 123 19128 638212 41963872
Hyperpyrexia 59.58 18.77 30 19221 3510 42598574
Vision blurred 59.09 18.77 95 19156 53604 42548480
Erythema nodosum 57.46 18.77 24 19227 1824 42600260
Metastases to lymph nodes 57.29 18.77 35 19216 5963 42596121
Metastases to peritoneum 57.21 18.77 26 19225 2423 42599661
Malignant melanoma 56.26 18.77 41 19210 9359 42592725
Haemophagocytic lymphohistiocytosis 53.99 18.77 53 19198 18169 42583915
Product use in unapproved indication 52.76 18.77 193 19058 184263 42417821
Blood lactate dehydrogenase increased 51.16 18.77 61 19190 26020 42576064
Drug ineffective 51.05 18.77 133 19118 630064 41972020
Drug interaction 50.49 18.77 29 19222 266970 42335114
Metastases to bone 49.43 18.77 46 19205 14763 42587321
Chorioretinopathy 47.99 18.77 20 19231 1511 42600573
Nausea 47.62 18.77 324 18927 396475 42205609
C-reactive protein increased 47.51 18.77 95 19156 63465 42538619
Metastases to meninges 46.38 18.77 21 19230 1940 42600144
Malignant mesenteric neoplasm 44.91 18.77 9 19242 41 42602043
Panniculitis 44.25 18.77 21 19230 2160 42599924
Metastases to skin 42.25 18.77 14 19237 554 42601530
Anaplastic thyroid cancer 41.14 18.77 7 19244 9 42602075
Toxicity to various agents 40.37 18.77 27 19224 229109 42372975
BRAF V600E mutation positive 40.00 18.77 8 19243 36 42602048
Hyperkeratosis 39.49 18.77 25 19226 4533 42597551
Metastasis 38.77 18.77 25 19226 4680 42597404
Intestinal metastasis 35.58 18.77 11 19240 347 42601737
Procalcitonin increased 34.57 18.77 18 19233 2258 42599826
Skin toxicity 33.49 18.77 26 19225 6523 42595561
Decreased appetite 32.88 18.77 173 19078 192964 42409120
Febrile neutropenia 32.53 18.77 22 19229 185681 42416403
Vogt-Koyanagi-Harada disease 32.51 18.77 9 19242 191 42601893
Brain neoplasm 31.99 18.77 20 19231 3548 42598536
Condition aggravated 31.60 18.77 43 19208 260711 42341373
Anxiety 30.40 18.77 8 19243 118552 42483532
Metastases to heart 29.39 18.77 8 19243 159 42601925
Overdose 29.17 18.77 6 19245 105258 42496826
Jejunal ulcer perforation 29.16 18.77 7 19244 82 42602002
Mesenteric neoplasm 29.16 18.77 6 19245 32 42602052
Concomitant disease aggravated 29.10 18.77 24 19227 6562 42595522
Vomiting 28.59 18.77 226 19025 289497 42312587
Asthenia 27.68 18.77 219 19032 280574 42321510
Papilloedema 25.94 18.77 17 19234 3269 42598815
Retinal detachment 25.18 18.77 22 19229 6503 42595581
Ureteral disorder 24.96 18.77 7 19244 156 42601928
Omental necrosis 24.57 18.77 5 19246 25 42602059
Headache 24.29 18.77 188 19063 239181 42362903
Hyperthermia 23.98 18.77 29 19222 12545 42589539
Eastern Cooperative Oncology Group performance status 23.66 18.77 5 19246 31 42602053
Gastrointestinal wall thickening 23.59 18.77 13 19238 1826 42600258
General physical health deterioration 23.37 18.77 132 19119 151114 42450970
Disease progression 23.27 18.77 127 19124 143529 42458555
Depression 22.62 18.77 11 19240 111352 42490732
Varicella virus test positive 22.14 18.77 7 19244 238 42601846
Dehydration 21.42 18.77 123 19128 141644 42460440
Left ventricular dysfunction 21.08 18.77 26 19225 11475 42590609
BRAF gene mutation 21.03 18.77 5 19246 56 42602028
Cerebral haemorrhage 20.89 18.77 51 19200 38915 42563169
Dysphagia 20.65 18.77 76 19175 72643 42529441
Drug hypersensitivity 19.91 18.77 10 19241 99379 42502705
Therapeutic product effect incomplete 19.74 18.77 4 19247 70935 42531149
Hepatitis 19.42 18.77 40 19211 27260 42574824
Body temperature fluctuation 19.38 18.77 11 19240 1636 42600448
Vitiligo 19.36 18.77 10 19241 1233 42600851
Lymphadenopathy 19.32 18.77 45 19206 33320 42568764
Tumour invasion 19.17 18.77 7 19244 371 42601713
Blood alkaline phosphatase increased 19.11 18.77 45 19206 33552 42568532
Metastases to pleura 18.96 18.77 8 19243 623 42601461
Brain neoplasm malignant 18.90 18.77 9 19242 932 42601152
Iridocyclitis 18.84 18.77 12 19239 2199 42599885
Leukoderma 18.83 18.77 5 19246 90 42601994

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 2489.53 17.91 1966 27109 896299 109663925
Malignant neoplasm progression 1629.48 17.91 830 28245 173737 110386487
Chills 664.77 17.91 483 28592 190097 110370127
Metastases to central nervous system 600.98 17.91 226 28849 22591 110537633
Death 494.24 17.91 750 28325 698119 109862105
Uveitis 409.75 17.91 169 28906 21541 110538683
Ejection fraction decreased 358.43 17.91 187 28888 40693 110519531
Blood creatine phosphokinase increased 202.95 17.91 162 28913 72915 110487309
Panniculitis 192.29 17.91 90 28985 15492 110544732
Serous retinal detachment 154.55 17.91 43 29032 1629 110558595
Squamous cell carcinoma 151.94 17.91 81 28994 18382 110541842
Erythema nodosum 146.88 17.91 58 29017 6595 110553629
Hyperpyrexia 129.47 17.91 56 29019 8013 110552211
Metastatic malignant melanoma 120.51 17.91 42 29033 3367 110556857
Metastases to lung 117.28 17.91 74 29001 22989 110537235
Second primary malignancy 112.49 17.91 66 29009 18002 110542222
Metastases to liver 110.24 17.91 84 28991 35302 110524922
BRAF V600E mutation positive 108.75 17.91 19 29056 68 110560156
Skin toxicity 106.36 17.91 55 29020 11728 110548496
Blood lactate dehydrogenase increased 105.72 17.91 90 28985 44244 110515980
Haemophagocytic lymphohistiocytosis 105.16 17.91 78 28997 31481 110528743
Chorioretinopathy 99.68 17.91 33 29042 2262 110557962
Malignant melanoma 92.97 17.91 57 29018 16834 110543390
Vogt-Koyanagi-Harada disease 91.16 17.91 23 29052 593 110559631
Basal cell carcinoma 90.19 17.91 83 28992 45187 110515037
Rash 90.10 17.91 440 28635 820524 109739700
Off label use 89.20 17.91 162 28913 1500023 109060201
Melanoma recurrent 88.84 17.91 20 29055 311 110559913
Metastases to lymph nodes 88.58 17.91 53 29022 14979 110545245
Drug ineffective 83.61 17.91 172 28903 1520368 109039856
Dermatitis acneiform 83.34 17.91 48 29027 12647 110547577
Hyperkeratosis 83.03 17.91 43 29032 9196 110551028
Iridocyclitis 81.78 17.91 36 29039 5372 110554852
Drug hypersensitivity 80.01 17.91 12 29063 454078 110106146
Metastasis 78.70 17.91 40 29035 8227 110551997
Metastases to bone 77.49 17.91 65 29010 31307 110528917
Visual impairment 73.51 17.91 129 28946 134299 110425925
Condition aggravated 73.29 17.91 52 29023 734784 109825440
Vision blurred 69.50 17.91 123 28952 128899 110431325
Metastases to meninges 67.56 17.91 31 29044 5097 110555127
Retinal detachment 65.05 17.91 39 29036 11061 110549163
Metastases to peritoneum 64.90 17.91 31 29044 5579 110554645
Aspartate aminotransferase increased 63.50 17.91 134 28941 159802 110400422
Rheumatoid arthritis 60.08 17.91 5 29070 299608 110260616
Procalcitonin increased 58.12 17.91 26 29049 4030 110556194
Metastases to stomach 57.95 17.91 14 29061 300 110559924
Dehydration 56.75 17.91 182 28893 279329 110280895
Hyperthermia 54.45 17.91 45 29030 21227 110538997
Vomiting 54.34 17.91 417 28658 910258 109649966
Rash maculo-papular 53.87 17.91 81 28994 74141 110486083
Decreased appetite 51.99 17.91 255 28820 475591 110084633
Maternal exposure during pregnancy 51.81 17.91 4 29071 254879 110305345
Cutaneous sarcoidosis 49.75 17.91 14 29061 553 110559671
Blood alkaline phosphatase increased 48.08 17.91 75 29000 70860 110489364
Musculoskeletal stiffness 47.89 17.91 8 29067 279814 110280410
Pneumonitis 47.87 17.91 78 28997 76453 110483771
Malignant mesenteric neoplasm 47.84 17.91 9 29066 53 110560171
Sinusitis 47.54 17.91 10 29065 296678 110263546
Arthropathy 47.52 17.91 9 29066 287513 110272711
Metastases to skin 47.12 17.91 19 29056 2280 110557944
Rhabdomyolysis 46.76 17.91 100 28975 120301 110439923
Disease progression 46.02 17.91 155 28920 243879 110316345
Joint swelling 45.88 17.91 30 29045 442815 110117409
C-reactive protein increased 45.22 17.91 143 28932 217776 110342448
Wheezing 44.34 17.91 7 29068 255223 110305001
Nausea 44.10 17.91 507 28568 1235183 109325041
Alanine aminotransferase increased 43.19 17.91 126 28949 183647 110376577
Sarcoid-like reaction 42.49 17.91 11 29064 315 110559909
Gamma-glutamyltransferase increased 41.80 17.91 65 29010 61244 110498980
Therapeutic product effect incomplete 41.56 17.91 5 29070 223800 110336424
Weight increased 41.37 17.91 30 29045 419614 110140610
BRAF gene mutation 40.85 17.91 8 29067 60 110560164
Drug interaction 40.57 17.91 43 29032 500140 110060084
Anxiety 40.57 17.91 20 29055 345058 110215166
Nasopharyngitis 40.46 17.91 27 29048 394334 110165890
Psoriatic arthropathy 40.23 17.91 3 29072 196758 110363466
Product use in unapproved indication 40.08 17.91 227 28848 447150 110113074
Overdose 39.31 17.91 7 29068 233787 110326437
Palmar-plantar erythrodysaesthesia syndrome 39.05 17.91 51 29024 40974 110519250
Intentional product use issue 38.41 17.91 9 29066 247897 110312327
Hypersensitivity 38.39 17.91 30 29045 403968 110156256
Myalgia 38.23 17.91 137 28938 222244 110337980
Impaired healing 37.52 17.91 4 29071 196713 110363511
Demyelinating polyneuropathy 37.36 17.91 16 29059 2233 110557991
Acute polyneuropathy 37.22 17.91 12 29063 756 110559468
Asthenia 36.91 17.91 308 28767 688691 109871533
Helicobacter infection 36.55 17.91 3 29072 181874 110378350
Fatigue 36.06 17.91 482 28593 1215476 109344748
Swelling 36.05 17.91 24 29051 351017 110209207
Metastases to adrenals 35.47 17.91 14 29061 1589 110558635
Visual acuity reduced 35.40 17.91 43 29032 32130 110528094
Squamous cell carcinoma of skin 35.15 17.91 32 29043 17171 110543053
Concomitant disease aggravated 34.54 17.91 31 29044 16333 110543891
Mobility decreased 34.16 17.91 10 29065 237412 110322812
Detachment of retinal pigment epithelium 34.06 17.91 12 29063 993 110559231
Toxicity to various agents 33.98 17.91 46 29029 480509 110079715
Keratoacanthoma 33.28 17.91 13 29062 1435 110558789
Lymphadenopathy 33.25 17.91 60 29015 63775 110496449
Product dose omission issue 33.04 17.91 22 29053 321760 110238464
Injury 32.81 17.91 4 29071 177261 110382963
Metastatic neoplasm 32.78 17.91 20 29055 5853 110554371
Disseminated intravascular coagulation 32.76 17.91 47 29028 41239 110518985
Hepatocellular injury 32.19 17.91 52 29023 50590 110509634
Osteoarthritis 31.74 17.91 5 29070 182618 110377606
Brain oedema 31.70 17.91 40 29035 31058 110529166
Hypophysitis 31.66 17.91 19 29056 5396 110554828
Papilloedema 30.89 17.91 21 29054 7388 110552836
Jejunal ulcer perforation 30.51 17.91 7 29068 119 110560105
Type 2 diabetes mellitus 30.47 17.91 5 29070 177227 110382997
Blood cholesterol increased 30.06 17.91 6 29069 184779 110375445
Cerebral haemorrhage 30.01 17.91 58 29017 64910 110495314
Hepatotoxicity 29.78 17.91 57 29018 63343 110496881
Treatment failure 29.77 17.91 18 29057 277216 110283008
Erythema multiforme 29.64 17.91 32 29043 21065 110539159
Lipase increased 29.22 17.91 30 29045 18642 110541582
Dysphagia 28.44 17.91 97 28978 153503 110406721
Intestinal metastasis 28.34 17.91 9 29066 540 110559684
Acquired gene mutation 28.19 17.91 14 29061 2740 110557484
Insomnia 28.12 17.91 32 29043 360558 110199666
Erysipelas 27.91 17.91 25 29050 13133 110547091
Tumour invasion 27.84 17.91 9 29066 572 110559652
Discomfort 27.49 17.91 11 29064 214696 110345528
Abdominal lymphadenopathy 27.09 17.91 12 29063 1816 110558408
Retinopathy 27.09 17.91 16 29059 4413 110555811
Non-small cell lung cancer recurrent 26.95 17.91 7 29068 203 110560021
Wound 26.92 17.91 14 29061 234423 110325801
Therapy partial responder 26.25 17.91 40 29035 37021 110523203
Influenza like illness 26.15 17.91 66 29009 88346 110471878
Autoimmune colitis 26.15 17.91 12 29063 1973 110558251
Mesenteric neoplasm 26.04 17.91 6 29069 104 110560120
Cholestasis 25.52 17.91 54 29021 64464 110495760
Blister 25.49 17.91 14 29061 227362 110332862
Paronychia 25.40 17.91 22 29053 11059 110549165
Hepatitis 25.37 17.91 66 29009 89988 110470236
Omental necrosis 25.25 17.91 5 29070 40 110560184
Serous retinopathy 25.08 17.91 7 29068 268 110559956
Amylase increased 25.01 17.91 23 29052 12496 110547728
Malignant melanoma stage IV 24.73 17.91 6 29069 131 110560093
Intentional overdose 24.50 17.91 3 29072 132498 110427726
Vitiligo 24.15 17.91 13 29062 3004 110557220
Body temperature fluctuation 24.06 17.91 14 29061 3759 110556465
Ureteral disorder 23.66 17.91 8 29067 585 110559639
Left ventricular dysfunction 23.60 17.91 30 29045 23463 110536761
Blood pressure increased 23.51 17.91 20 29055 258353 110301871
Therapy cessation 23.16 17.91 42 29033 44815 110515409
Panniculitis lobular 22.97 17.91 5 29070 66 110560158
Transaminases increased 22.73 17.91 51 29024 63339 110496885
Macular oedema 22.71 17.91 17 29058 6949 110553275
Varicella virus test positive 22.46 17.91 7 29068 395 110559829
Pain 22.46 17.91 153 28922 954802 109605422
Seizure 22.31 17.91 116 28959 221069 110339155
Tumour haemorrhage 22.18 17.91 15 29060 5230 110554994
Metastases to heart 21.96 17.91 7 29068 425 110559799
Hepatic function abnormal 21.71 17.91 62 29013 89233 110470991
Migraine 21.64 17.91 9 29066 171643 110388581
Abdominal discomfort 21.11 17.91 45 29030 393813 110166411
Chest pain 21.02 17.91 42 29033 376333 110183891
Fall 20.71 17.91 85 28990 603397 109956827
Vitreous floaters 20.66 17.91 18 29057 9116 110551108
Intracranial pressure increased 20.36 17.91 19 29056 10516 110549708
Metastases to thorax 20.27 17.91 6 29069 284 110559940
Guillain-Barre syndrome 20.04 17.91 19 29056 10725 110549499
Depression 19.87 17.91 33 29042 317302 110242922
Sleep disorder 19.82 17.91 14 29061 198630 110361594
Drug resistance 19.81 17.91 45 29030 56329 110503895
Drug intolerance 19.72 17.91 49 29026 406463 110153761
Brain neoplasm 19.63 17.91 15 29060 6322 110553902
Metastases to spine 19.60 17.91 14 29061 5329 110554895
General physical health deterioration 19.55 17.91 184 28891 425111 110135113
Nodular rash 19.40 17.91 6 29069 330 110559894
Gastrointestinal wall thickening 19.36 17.91 12 29063 3611 110556613
Sarcoidosis 19.31 17.91 20 29055 12559 110547665
Eastern Cooperative Oncology Group performance status 19.29 17.91 5 29070 144 110560080
Urticaria 19.19 17.91 34 29041 318823 110241401
Polyneuropathy 19.16 17.91 32 29043 31980 110528244
Bacterial diarrhoea 18.83 17.91 6 29069 364 110559860
Itching scar 18.58 17.91 4 29071 50 110560174
Body temperature increased 18.49 17.91 43 29032 54670 110505554
Facial paralysis 18.38 17.91 27 29048 24187 110536037
Intestinal perforation 18.34 17.91 25 29050 20919 110539305
Psoriasis 18.20 17.91 7 29068 139986 110420238
Peripheral motor neuropathy 18.04 17.91 12 29063 4074 110556150

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 agent
CHEBI has role CHEBI:75047 B-Raf inhibitor
CHEBI has role CHEBI:149553 anticoronaviral agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L01EC B-Raf serine-threonine kinase (BRAF) inhibitors 3 drugs
encorafenibtovorafenibvemurafenib

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 9233956 May 4, 2029 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8952018 Oct. 15, 2030 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8952018 Oct. 15, 2030 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 10MG BASE TAFINLAR NOVARTIS N217514 March 16, 2023 RX TABLET, FOR SUSPENSION ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 10869869 Aug. 30, 2033 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 10869869 Aug. 30, 2033 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL March 16, 2026 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL March 16, 2026 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 10MG BASE TAFINLAR NOVARTIS N217514 March 16, 2023 RX TABLET, FOR SUSPENSION ORAL March 16, 2026 NEW PRODUCT
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 10MG BASE TAFINLAR NOVARTIS N217514 March 16, 2023 RX TABLET, FOR SUSPENSION ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL March 16, 2030 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL March 16, 2030 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 10MG BASE TAFINLAR NOVARTIS N217514 March 16, 2023 RX TABLET, FOR SUSPENSION ORAL March 16, 2030 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY
EQ 10MG BASE TAFINLAR NOVARTIS N217514 March 16, 2023 RX TABLET, FOR SUSPENSION ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY

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
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
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor EC50 7.06 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
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
9458 INN_ID
44462760 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-0681 CAPSULE 75 mg ORAL NDA 33 sections
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-0682 CAPSULE 50 mg ORAL NDA 33 sections
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-1154 TABLET, FOR SUSPENSION 10 mg ORAL NDA 33 sections