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

Stem definitionDrug idCAS RN
MEK (MAPK kinase) tyrosine kinase inhibitors 4802 871700-17-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • GSK1120212B
  • trametinib dimethyl sulfoxide
  • trametinib
  • GSK1120212
  • mekinist
a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation
  • Molecular weight: 615.40
  • Formula: C26H23FIN5O4
  • CLOGP: 4.68
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 102.06
  • ALOGS: -4.30
  • ROTB: 5

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 13.94 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.03 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 229 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 29, 2013 FDA NOVARTIS PHARMS CORP
March 28, 2016 PMDA Novartis Pharma K.K.
June 30, 2014 EMA NOVARTIS EUROPHARM LIMITED

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 1326.38 18.99 1053 16096 469425 63002448
Malignant neoplasm progression 1021.03 18.99 479 16670 81642 63390231
Chills 372.09 18.99 280 16869 113098 63358775
Product use in unapproved indication 335.15 18.99 320 16829 178760 63293113
Death 299.65 18.99 432 16717 373949 63097924
Uveitis 225.26 18.99 95 17054 12458 63459415
Visual impairment 196.93 18.99 171 16978 84275 63387598
Metastases to central nervous system 188.91 18.99 85 17064 13020 63458853
Rash 183.09 18.99 440 16709 560431 62911442
Ejection fraction decreased 135.58 18.99 81 17068 22251 63449622
Dermatitis acneiform 124.85 18.99 48 17101 4948 63466925
Panniculitis 124.41 18.99 61 17088 11324 63460549
Blood creatine phosphokinase increased 112.70 18.99 81 17068 30349 63441524
Skin toxicity 92.36 18.99 38 17111 4676 63467197
Drug ineffective 84.81 18.99 95 17054 1044670 62427203
Vision blurred 77.28 18.99 109 17040 91815 63380058
Erythema nodosum 71.44 18.99 32 17117 4843 63467030
Paronychia 70.47 18.99 33 17116 5532 63466341
Serous retinal detachment 65.45 18.99 16 17133 351 63471522
Chorioretinopathy 65.39 18.99 19 17130 820 63471053
Dry skin 56.22 18.99 73 17076 56814 63415059
Acne 53.85 18.99 47 17102 23246 63448627
Metastatic malignant melanoma 53.02 18.99 18 17131 1297 63470576
Drug hypersensitivity 52.81 18.99 10 17139 310677 63161196
Condition aggravated 51.73 18.99 22 17127 402195 63069678
Vogt-Koyanagi-Harada disease 50.12 18.99 11 17138 147 63471726
Haemophagocytic lymphohistiocytosis 45.66 18.99 31 17118 10596 63461277
Aspartate aminotransferase increased 45.63 18.99 85 17064 90192 63381681
Nausea 45.61 18.99 389 16760 854082 62617791
Lipase increased 45.22 18.99 30 17119 9870 63462003
BRAF V600E mutation positive 44.87 18.99 8 17141 32 63471841
Detachment of retinal pigment epithelium 44.75 18.99 12 17137 384 63471489
Hyperpyrexia 44.33 18.99 21 17128 3611 63468262
Second primary malignancy 43.51 18.99 27 17122 7926 63463947
Diarrhoea 43.16 18.99 335 16814 715031 62756842
Metastases to lung 42.80 18.99 32 17117 12718 63459155
Blood lactate dehydrogenase increased 42.44 18.99 41 17108 23075 63448798
Sinusitis 41.37 18.99 6 17143 226647 63245226
Metastasis 39.96 18.99 22 17127 5175 63466698
Erythema multiforme 39.78 18.99 28 17121 10141 63461732
Arthropathy 38.95 18.99 8 17141 234784 63237089
Vomiting 38.79 18.99 271 16878 559346 62912527
Rash maculo-papular 38.04 18.99 45 17104 31851 63440022
Dehydration 37.11 18.99 117 17032 173237 63298636
Glossodynia 37.04 18.99 3 17146 178873 63293000
Metastases to meninges 34.71 18.99 16 17133 2586 63469287
Fall 34.63 18.99 33 17116 392301 63079572
Wound 33.09 18.99 3 17146 163260 63308613
Pneumonitis 32.93 18.99 44 17105 35178 63436695
Non-small cell lung cancer recurrent 32.22 18.99 7 17142 89 63471784
Iridocyclitis 32.07 18.99 15 17134 2507 63469366
Discomfort 31.56 18.99 4 17145 167370 63304503
Rhabdomyolysis 30.97 18.99 48 17101 43903 63427970
Abdominal discomfort 30.70 18.99 25 17124 320860 63151013
Systemic inflammatory response syndrome 30.54 18.99 19 17130 5602 63466271
Malignant melanoma 30.53 18.99 25 17124 11331 63460542
Alanine aminotransferase increased 29.93 18.99 78 17071 103692 63368181
Vitreous floaters 29.50 18.99 19 17130 5947 63465926
Retinal detachment 29.49 18.99 19 17130 5950 63465923
Erysipelas 29.15 18.99 21 17128 7884 63463989
Melanoma recurrent 28.79 18.99 7 17142 150 63471723
Metastases to peritoneum 27.65 18.99 15 17134 3427 63468446
Joint swelling 27.25 18.99 29 17120 327637 63144236
Musculoskeletal stiffness 25.51 18.99 9 17140 184609 63287264
Disease progression 25.47 18.99 82 17067 122676 63349197
Serous retinopathy 25.45 18.99 5 17144 37 63471836
Weight increased 25.34 18.99 20 17129 260772 63211101
Panniculitis lobular 25.22 18.99 5 17144 39 63471834
Chest pain 24.41 18.99 14 17135 215945 63255928
Metastases to liver 24.38 18.99 31 17118 23608 63448265
Hypersensitivity 24.23 18.99 26 17123 292659 63179214
Sepsis 23.80 18.99 93 17056 153030 63318843
Metastases to spleen 23.43 18.99 6 17143 160 63471713
Immune-mediated hepatitis 23.33 18.99 10 17139 1361 63470512
Swelling 23.31 18.99 24 17125 275354 63196519
Insomnia 22.87 18.99 15 17134 215237 63256636
Metastases to lymph nodes 22.02 18.99 18 17131 8140 63463733
Leukoderma 21.77 18.99 5 17144 83 63471790
Nasopharyngitis 21.70 18.99 22 17127 254235 63217638
C-reactive protein increased 21.24 18.99 65 17084 94642 63377231
Sarcoid-like reaction 20.95 18.99 4 17145 25 63471848
Pancreatitis 20.90 18.99 43 17106 49012 63422861
Hepatitis 20.76 18.99 38 17111 39750 63432123
Acute polyneuropathy 20.65 18.99 6 17143 259 63471614
Drug interaction 20.51 18.99 19 17130 229112 63242761
Infective glossitis 19.67 18.99 4 17145 36 63471837
Treatment failure 19.66 18.99 15 17134 199028 63272845
Metastatic neoplasm 19.58 18.99 13 17136 4282 63467591
Decreased appetite 19.36 18.99 125 17024 250927 63220946
Transaminases increased 19.01 18.99 32 17117 31335 63440538

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 1272.24 17.89 1149 16212 331864 34607706
Malignant neoplasm progression 820.29 17.89 521 16840 87525 34852045
Metastases to central nervous system 395.56 17.89 150 17211 8055 34931515
Chills 379.70 17.89 317 17044 80726 34858844
Death 251.77 17.89 585 16776 397464 34542106
Product use in unapproved indication 195.59 17.89 265 17096 117234 34822336
Ejection fraction decreased 186.46 17.89 117 17244 19037 34920533
Rash 132.87 17.89 321 17040 222431 34717139
Visual impairment 121.50 17.89 117 17244 35685 34903885
Uveitis 118.72 17.89 63 17298 7472 34932098
Blood creatine phosphokinase increased 109.73 17.89 123 17238 44734 34894836
Metastases to liver 86.50 17.89 64 17297 13599 34925971
Dermatitis acneiform 81.59 17.89 46 17315 6143 34933427
Second primary malignancy 73.76 17.89 47 17314 7839 34931731
Metastases to stomach 71.64 17.89 15 17346 79 34939491
Metastases to lung 68.95 17.89 48 17313 9272 34930298
Melanoma recurrent 64.46 17.89 15 17346 137 34939433
Acne 63.75 17.89 49 17312 11017 34928553
Chorioretinopathy 63.71 17.89 25 17336 1468 34938102
Drug interaction 59.72 17.89 19 17342 225927 34713643
Hyperpyrexia 54.60 17.89 27 17334 2761 34936809
Malignant melanoma 53.69 17.89 39 17322 8051 34931519
Metastatic malignant melanoma 52.82 17.89 24 17337 2031 34937539
Blood lactate dehydrogenase increased 51.04 17.89 60 17301 22930 34916640
Haemophagocytic lymphohistiocytosis 48.95 17.89 45 17316 12928 34926642
Vision blurred 48.38 17.89 84 17277 45879 34893691
C-reactive protein increased 47.00 17.89 91 17270 54007 34885563
Paronychia 44.05 17.89 25 17336 3380 34936190
Serous retinal detachment 43.80 17.89 15 17346 597 34938973
Metastases to lymph nodes 43.77 17.89 28 17333 4700 34934870
Fatigue 41.00 17.89 319 17042 370334 34569236
Metastases to meninges 40.62 17.89 18 17343 1436 34938134
Toxicity to various agents 40.13 17.89 25 17336 200337 34739233
Metastases to peritoneum 39.54 17.89 19 17342 1825 34937745
Metastases to bone 38.47 17.89 38 17323 11932 34927638
Detachment of retinal pigment epithelium 38.21 17.89 13 17348 507 34939063
Malignant mesenteric neoplasm 37.91 17.89 8 17353 44 34939526
Metastases to skin 35.98 17.89 12 17349 440 34939130
Off label use 35.29 17.89 100 17261 419424 34520146
Drug ineffective 34.77 17.89 114 17247 456637 34482933
Procalcitonin increased 34.42 17.89 17 17344 1734 34937836
Skin toxicity 33.89 17.89 24 17337 4760 34934810
Jejunal ulcer perforation 33.20 17.89 8 17353 86 34939484
Panniculitis 32.33 17.89 17 17344 1977 34937593
Metastasis 32.19 17.89 22 17339 4122 34935448
Squamous cell carcinoma 30.68 17.89 33 17328 11442 34928128
Decreased appetite 29.87 17.89 162 17199 166230 34773340
Intestinal metastasis 29.47 17.89 9 17352 247 34939323
Metastases to heart 29.23 17.89 8 17353 147 34939423
Omental necrosis 28.91 17.89 6 17355 30 34939540
Anxiety 28.76 17.89 7 17354 99421 34840149
Condition aggravated 28.60 17.89 32 17329 192164 34747406
Mesenteric neoplasm 28.59 17.89 6 17355 32 34939538
Tissue infiltration 28.58 17.89 7 17354 81 34939489
Vomiting 28.33 17.89 215 17146 247406 34692164
Gastrointestinal wall thickening 27.84 17.89 14 17347 1484 34938086
Basal cell carcinoma 27.63 17.89 41 17320 19617 34919953
Ureteral disorder 27.62 17.89 8 17353 182 34939388
Eastern Cooperative Oncology Group performance status 27.58 17.89 6 17355 39 34939531
Overdose 27.15 17.89 6 17355 91053 34848517
Retinal detachment 27.03 17.89 22 17339 5369 34934201
Dehydration 26.40 17.89 131 17230 129838 34809732
Brain neoplasm 24.84 17.89 17 17344 3192 34936378
Nausea 24.04 17.89 266 17095 339642 34599928
Dry skin 24.01 17.89 50 17311 31237 34908333
Influenza like illness 23.39 17.89 46 17315 27588 34911982
Erythema nodosum 22.93 17.89 12 17349 1382 34938188
Depression 22.53 17.89 10 17351 97088 34842482
Papilloedema 22.50 17.89 15 17346 2698 34936872
Febrile neutropenia 22.37 17.89 21 17340 136828 34802742
Abdominal lymphadenopathy 22.03 17.89 10 17351 844 34938726
Left ventricular dysfunction 22.01 17.89 26 17335 9981 34929589
Concomitant disease aggravated 21.94 17.89 20 17341 5681 34933889
Myocardial infarction 21.71 17.89 17 17344 121068 34818502
Dermatitis 21.49 17.89 25 17336 9443 34930127
General physical health deterioration 21.08 17.89 122 17239 128147 34811423
BRAF gene mutation 20.64 17.89 5 17356 55 34939515
Metastases to adrenals 20.41 17.89 10 17351 1002 34938568
Fat necrosis 20.08 17.89 7 17354 294 34939276
Liver function test increased 19.92 17.89 30 17331 14535 34925035
Tumour invasion 19.83 17.89 7 17354 305 34939265
Blood alkaline phosphatase increased 19.60 17.89 46 17315 31129 34908441
Therapy partial responder 19.54 17.89 24 17337 9592 34929978
Cerebral haemorrhage 19.25 17.89 49 17312 34888 34904682
Leukoderma 19.03 17.89 5 17356 78 34939492
Blood pressure increased 19.03 17.89 10 17351 88092 34851478
Brain neoplasm malignant 18.92 17.89 9 17352 845 34938725
Retinopathy 18.55 17.89 12 17349 2052 34937518
Iridocyclitis 18.38 17.89 11 17350 1641 34937929
Small intestine carcinoma 18.15 17.89 8 17353 630 34938940
Pneumonitis 18.13 17.89 47 17314 33831 34905739
General physical condition abnormal 17.99 17.89 15 17346 3784 34935786

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 1929.60 16.52 1694 25864 677015 79039815
Malignant neoplasm progression 1456.73 16.52 776 26782 135214 79581616
Chills 478.62 16.52 415 27143 159819 79557011
Metastases to central nervous system 438.59 16.52 177 27381 16198 79700632
Death 361.73 16.52 676 26882 565838 79150992
Ejection fraction decreased 326.13 16.52 182 27376 34395 79682435
Uveitis 273.79 16.52 128 27430 16702 79700128
Product use in unapproved indication 225.53 16.52 349 27209 250010 79466820
Blood creatine phosphokinase increased 208.71 16.52 177 27381 65913 79650917
Dermatitis acneiform 181.29 16.52 82 27476 9911 79706919
Rash 145.41 16.52 484 27074 577874 79138956
Chorioretinopathy 126.71 16.52 42 27516 2189 79714641
Panniculitis 110.83 16.52 63 27495 12308 79704522
Paronychia 104.59 16.52 52 27506 7756 79709074
Blood lactate dehydrogenase increased 101.82 16.52 94 27464 39076 79677754
Serous retinal detachment 98.87 16.52 29 27529 1005 79715825
Metastases to lung 97.99 16.52 67 27491 18096 79698734
Second primary malignancy 97.11 16.52 61 27497 14289 79702541
Haemophagocytic lymphohistiocytosis 95.77 16.52 71 27487 21766 79695064
Metastases to liver 93.79 16.52 78 27480 28236 79688594
Hyperpyrexia 88.86 16.52 43 27515 6049 79710781
Detachment of retinal pigment epithelium 87.41 16.52 25 27533 791 79716039
Drug ineffective 85.77 16.52 152 27406 1080761 78636069
Skin toxicity 84.48 16.52 46 27512 8268 79708562
Melanoma recurrent 81.97 16.52 19 27539 253 79716577
Erythema nodosum 75.95 16.52 37 27521 5280 79711550
Visual impairment 73.87 16.52 122 27436 92009 79624821
Condition aggravated 73.43 16.52 41 27517 501083 79215747
Metastatic malignant melanoma 73.36 16.52 30 27528 2833 79713997
C-reactive protein increased 69.58 16.52 144 27414 128883 79587947
Malignant melanoma 69.33 16.52 50 27508 14691 79702139
Metastasis 66.96 16.52 37 27521 6843 79709987
Drug hypersensitivity 65.62 16.52 12 27546 298904 79417926
Metastases to lymph nodes 64.89 16.52 42 27516 10355 79706475
Metastases to peritoneum 64.19 16.52 31 27527 4341 79712489
Drug interaction 63.69 16.52 32 27526 415151 79301679
Metastases to stomach 60.13 16.52 15 27543 277 79716553
Aspartate aminotransferase increased 59.27 16.52 141 27417 138500 79578330
Dehydration 58.78 16.52 204 27354 247983 79468847
Procalcitonin increased 58.77 16.52 26 27532 2980 79713850
Squamous cell carcinoma 57.98 16.52 46 27512 15576 79701254
Metastases to meninges 57.34 16.52 27 27531 3574 79713256
Rheumatoid arthritis 56.56 16.52 4 27554 208466 79508364
Lipase increased 55.85 16.52 46 27512 16420 79700410
Retinal detachment 54.40 16.52 36 27522 9211 79707619
Toxicity to various agents 52.90 16.52 41 27517 421499 79295331
BRAF V600E mutation positive 52.86 16.52 10 27548 44 79716786
Rash maculo-papular 51.46 16.52 79 27479 55999 79660831
Iridocyclitis 50.59 16.52 25 27533 3679 79713151
Metastases to bone 49.21 16.52 51 27507 24376 79692454
Vogt-Koyanagi-Harada disease 47.34 16.52 12 27546 237 79716593
Vomiting 46.88 16.52 391 27167 665437 79051393
Vision blurred 45.57 16.52 108 27450 105790 79611040
Dry skin 45.30 16.52 83 27475 67912 79648918
Sinusitis 44.76 16.52 7 27551 195494 79521336
Metastases to skin 43.80 16.52 18 27540 1721 79715109
Pneumonitis 42.72 16.52 76 27482 60784 79656046
Decreased appetite 42.08 16.52 231 27327 342187 79374643
Malignant mesenteric neoplasm 39.53 16.52 8 27550 53 79716777
BRAF gene mutation 38.79 16.52 8 27550 59 79716771
Alanine aminotransferase increased 37.90 16.52 133 27425 162437 79554393
Blood alkaline phosphatase increased 37.81 16.52 74 27484 63590 79653240
Off label use 37.42 16.52 174 27384 907041 78809789
Overdose 37.11 16.52 9 27549 184197 79532633
Therapy partial responder 36.26 16.52 37 27521 17360 79699470
Anxiety 35.38 16.52 21 27537 248491 79468339
Joint swelling 35.02 16.52 29 27529 288617 79428213
Therapeutic product effect incomplete 34.97 16.52 4 27554 141641 79575189
Metastases to adrenals 34.29 16.52 14 27544 1316 79715514
Abdominal lymphadenopathy 34.25 16.52 14 27544 1320 79715510
Jejunal ulcer perforation 33.44 16.52 8 27550 123 79716707
Basal cell carcinoma 33.37 16.52 52 27506 37323 79679507
Intestinal metastasis 33.31 16.52 10 27548 376 79716454
Product dose omission issue 32.40 16.52 23 27535 247514 79469316
Arthropathy 31.37 16.52 11 27547 177100 79539730
Weight increased 31.09 16.52 30 27528 277356 79439474
Musculoskeletal stiffness 30.78 16.52 11 27547 174997 79541833
Fall 30.58 16.52 78 27480 487551 79229279
Nasopharyngitis 30.18 16.52 26 27532 253855 79462975
Dermatitis 30.09 16.52 37 27521 21284 79695546
Insomnia 29.28 16.52 25 27533 245145 79471685
Visual acuity reduced 29.14 16.52 43 27515 29426 79687404
Omental necrosis 29 16.52 6 27552 45 79716785
Blood pressure increased 28.51 16.52 19 27539 211341 79505489
Non-small cell lung cancer recurrent 28.49 16.52 7 27551 121 79716709
Eastern Cooperative Oncology Group performance status 28.44 16.52 6 27552 50 79716780
Erysipelas 28.11 16.52 26 27532 10824 79706006
Demyelinating polyneuropathy 27.66 16.52 13 27545 1713 79715117
Retinopathy 27.48 16.52 17 27541 3874 79712956
Concomitant disease aggravated 27.44 16.52 28 27530 13139 79703691
Acne 27.36 16.52 40 27518 27150 79689680
Cutaneous sarcoidosis 27.24 16.52 9 27549 464 79716366
Mesenteric neoplasm 26.94 16.52 6 27552 66 79716764
Acute polyneuropathy 26.93 16.52 9 27549 481 79716349
Hypophysitis 26.41 16.52 17 27541 4149 79712681
Treatment failure 26.31 16.52 13 27545 170473 79546357
Vitreous floaters 26.14 16.52 21 27537 7235 79709595
Intentional overdose 26.13 16.52 3 27555 105957 79610873
Intestinal perforation 25.83 16.52 31 27527 17395 79699435
Nausea 25.53 16.52 468 27090 956728 78760102
Amylase increased 25.50 16.52 25 27533 11184 79705646
Disease progression 25.09 16.52 128 27430 184234 79532596
Gastrointestinal wall thickening 25.06 16.52 14 27544 2643 79714187
Gamma-glutamyltransferase increased 24.86 16.52 57 27501 54623 79662207
Tumour invasion 24.61 16.52 8 27550 392 79716438
Mobility decreased 24.54 16.52 6 27552 122169 79594661
Hypersensitivity 24.35 16.52 33 27525 262206 79454624
Therapy cessation 23.94 16.52 45 27513 37517 79679313
Erythema multiforme 23.90 16.52 30 27528 17621 79699209
Rhabdomyolysis 23.70 16.52 84 27474 103047 79613783
Metastatic neoplasm 23.47 16.52 17 27541 5025 79711805
Peritoneal disorder 23.36 16.52 9 27549 726 79716104
Left ventricular dysfunction 23.23 16.52 31 27527 19330 79697500
Wheezing 22.91 16.52 6 27552 116658 79600172
Chest pain 22.86 16.52 39 27519 282265 79434565
Metastases to pleura 22.76 16.52 11 27547 1543 79715287
Metastases to heart 22.71 16.52 7 27551 288 79716542
Squamous cell carcinoma of skin 22.52 16.52 26 27532 14007 79702823
Papilloedema 22.37 16.52 18 27540 6215 79710615
Pancreatitis 22.32 16.52 63 27495 68512 79648318
Autoimmune colitis 22.30 16.52 11 27547 1612 79715218
Serous retinopathy 22.14 16.52 6 27552 155 79716675
Abdominal discomfort 21.84 16.52 33 27525 250694 79466136
Cerebral haemorrhage 21.81 16.52 56 27502 57617 79659213
Ureteral disorder 21.79 16.52 8 27550 565 79716265
Rash pustular 21.68 16.52 23 27535 11288 79705542
Influenza like illness 21.53 16.52 64 27494 71643 79645187
Lymphadenopathy 21.49 16.52 53 27505 53194 79663636
General physical health deterioration 21.10 16.52 165 27393 275073 79441757
Pancreatic enzymes increased 21.01 16.52 10 27548 1355 79715475
Hypoalbuminaemia 20.95 16.52 31 27527 21266 79695564
Metastases to spleen 20.88 16.52 8 27550 636 79716194
Pain 20.88 16.52 150 27408 703652 79013178
Depression 20.41 16.52 27 27531 216763 79500067
Intentional product use issue 20.07 16.52 14 27544 152098 79564732
Macular oedema 20.06 16.52 16 27542 5458 79711372
Drug intolerance 20.03 16.52 38 27520 264081 79452749
Hepatocellular injury 19.88 16.52 48 27510 47545 79669285
Hepatotoxicity 19.56 16.52 50 27508 51302 79665528
Tumour haemorrhage 19.35 16.52 14 27544 4130 79712700
Transaminases increased 19.31 16.52 50 27508 51693 79665137
Chest discomfort 19.17 16.52 12 27546 138032 79578798
Xerosis 19.07 16.52 9 27549 1197 79715633
COVID-19 18.91 16.52 16 27542 157658 79559172
Brain neoplasm malignant 18.86 16.52 10 27548 1703 79715127
Hyperthermia 18.82 16.52 27 27531 18010 79698820
Psoriasis 18.79 16.52 4 27554 89583 79627247
Discomfort 18.75 16.52 10 27548 125607 79591223
Liver function test increased 18.67 16.52 42 27516 39731 79677099
Sarcoid-like reaction 18.59 16.52 4 27554 37 79716793
Swelling 18.42 16.52 29 27529 216682 79500148
Asthenia 17.58 16.52 261 27297 511428 79205402
Panniculitis lobular 17.56 16.52 4 27554 49 79716781
Fatigue 17.42 16.52 432 27126 929295 78787535
Small intestine carcinoma 17.21 16.52 8 27550 1028 79715802
Leukoderma 17.16 16.52 5 27553 169 79716661
Hyperkeratosis 17.03 16.52 17 27541 7773 79709057
Hepatitis 16.98 16.52 50 27508 55677 79661153
Vitiligo 16.92 16.52 10 27548 2099 79714731
Tissue infiltration 16.89 16.52 7 27551 684 79716146
Eczema 16.87 16.52 41 27517 40777 79676053
Suicide attempt 16.79 16.52 4 27554 82928 79633902
Protein S increased 16.76 16.52 3 27555 9 79716821
Infective glossitis 16.75 16.52 4 27554 61 79716769
Intentional product misuse 16.69 16.52 6 27552 95159 79621671

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EE01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Mitogen-activated protein kinase (MEK) 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
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:79091 MEK inhibitor
CHEBI has role CHEBI:149553 anticoronaviral drug
CHEBI has role CHEBI:176497 geroprotectors

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

DiseaseRelationSNOMED_IDDOID
Locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation indication 255031003
Metastatic malignant melanoma indication 443493003
Malignant Melanoma with BRAF V600E Mutation indication 830150003
Malignant Melanoma with BRAF V600K Mutation indication
Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation indication
Unresectable or metastatic solid tumors with BRAF V600E mutation indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 MEKINIST 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8835443 June 10, 2025 TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8835443 June 10, 2025 TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL 8835443 June 10, 2025 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8952018 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 8952018 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 8952018 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL 8703781 Oct. 15, 2030 MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 10869869 Aug. 30, 2033 MEKINIST(R) 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL 10869869 Aug. 30, 2033 MEKINIST(R) 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL 10869869 Aug. 30, 2033 MEKINIST(R) 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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL June 22, 2024 TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL June 22, 2024 TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL June 22, 2024 TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Dec. 22, 2024 PEDIATRIC EXCLUSIVITY
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Dec. 22, 2024 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Dec. 22, 2024 PEDIATRIC EXCLUSIVITY
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL June 22, 2025 TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL June 22, 2025 TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL June 22, 2025 TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Oct. 30, 2025 PEDIATRIC EXCLUSIVITY
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Oct. 30, 2025 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Oct. 30, 2025 PEDIATRIC EXCLUSIVITY
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Nov. 4, 2025 PEDIATRIC EXCLUSIVITY
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Nov. 4, 2025 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Nov. 4, 2025 PEDIATRIC EXCLUSIVITY
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Dec. 22, 2025 PEDIATRIC EXCLUSIVITY
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Dec. 22, 2025 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Dec. 22, 2025 PEDIATRIC EXCLUSIVITY
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL March 16, 2026 NEW PRODUCT
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET 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 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL March 16, 2030 TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Dual specificity mitogen-activated protein kinase kinase 2 Kinase INHIBITOR IC50 9.04 WOMBAT-PK CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase INHIBITOR IC50 8.75 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter EC50 6.61 CHEMBL

External reference:

IDSource
D10175 KEGG_DRUG
1187431-43-1 SECONDARY_CAS_RN
4032511 VANDF
CHEBI:75998 CHEBI
QOM PDB_CHEM_ID
CHEMBL2103875 ChEMBL_ID
CHEMBL2105741 ChEMBL_ID
C560077 MESH_SUPPLEMENTAL_RECORD_UI
6495 IUPHAR_LIGAND_ID
9421 INN_ID
DB08911 DRUGBANK_ID
33E86K87QN UNII
1425098 RXNORM
203115 MMSL
29478 MMSL
41325 MMSL
d08104 MMSL
015044 NDDF
015045 NDDF
708711009 SNOMEDCT_US
715545006 SNOMEDCT_US
734611008 SNOMEDCT_US
C2697961 UMLSCUI
11707110 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0666 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0666 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0666 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0666 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0668 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0668 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0668 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0668 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1105 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1105 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1105 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1105 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1112 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1112 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1112 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1112 TABLET, FILM COATED 2 mg ORAL NDA 32 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-1161 POWDER, FOR SOLUTION 0.05 mg ORAL NDA 32 sections