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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.998 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.335 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 13.062 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.556 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.710 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 2.390 % High 1
herg hERG pIC50 5.090 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.926 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 7.638 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.610 % High 1
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AXL,BLK,BMX,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT3,FYN,GAK,GRK2,GSK3B,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK11,MAPK14,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TEK,TTK,ULK1,ULK2 68
kinase-selectivity-class ACVR2B,ALK,AURKA,AXL,BLK,BMX,BRAF,CAMK2D,CDK9,CSF1R,DDR1,ERBB2,ERBB4,GRK2,MAP2K1,MAP2K6,MAP3K21,MAP4K1,MAP4K3,MAPK1,MAPK7,MARK4,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TTK,ULK1 32
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 10.765 High 1
mh-clint Mouse hepatocyte intrinsic clearance 13.996 High 1
mppb Mouse plasma protein binding (% unbound) 0.450 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 20.654 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.560 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.729 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 3.090 % High 1
rppb Rat plasma protein binding (% unbound) 0.780 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1.803 uM High 1

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 1566.39 19.84 1290 21158 659195 89946804
Malignant neoplasm progression 1446.48 19.84 644 21804 106226 90499773
Chills 486.33 19.84 338 22110 131643 90474356
Death 407.28 19.84 531 21917 456020 90149979
Product use in unapproved indication 348.67 19.84 422 22026 335814 90270185
Visual impairment 297.85 19.84 253 22195 132112 90473887
Rash 275.34 19.84 606 21842 795494 89810505
Metastases to central nervous system 259.80 19.84 113 22335 17429 90588570
Uveitis 257.11 19.84 109 22339 15794 90590205
Dermatitis acneiform 201.13 19.84 71 22377 6283 90599716
Blood creatine phosphokinase increased 178.68 19.84 109 22339 33914 90572085
Panniculitis 175.34 19.84 81 22367 14377 90591622
Ejection fraction decreased 171.83 19.84 97 22351 26156 90579843
Metastatic malignant melanoma 167.73 19.84 45 22403 1579 90604420
Skin toxicity 152.75 19.84 59 22389 6720 90599279
Vision blurred 136.55 19.84 152 22296 110141 90495858
Acne 118.95 19.84 79 22369 28428 90577571
Paronychia 116.64 19.84 51 22397 7955 90598044
Erythema nodosum 101.77 19.84 42 22406 5682 90600317
Diarrhoea 95.88 19.84 472 21976 938718 89667281
Serous retinal detachment 81.98 19.84 21 22427 613 90605386
Nausea 77.50 19.84 504 21944 1109812 89496187
Rheumatoid arthritis 76.79 19.84 3 22445 362611 90243388
Maternal exposure during pregnancy 76.18 19.84 3 22445 360060 90245939
Dry skin 75.74 19.84 101 22347 87972 90518027
Ovarian cancer recurrent 75.04 19.84 24 22424 1566 90604433
Hyperpyrexia 74.83 19.84 32 22416 4729 90601270
Drug hypersensitivity 71.60 19.84 14 22434 463595 90142404
Metastases to lung 70.80 19.84 46 22402 15945 90590054
Chorioretinopathy 70.61 19.84 20 22428 860 90605139
Condition aggravated 70.04 19.84 30 22418 595515 90010484
BRAF V600E mutation positive 69.39 19.84 12 22436 43 90605956
Glossodynia 67.00 19.84 3 22445 321776 90284223
Vogt-Koyanagi-Harada disease 64.91 19.84 16 22432 398 90605601
Arthropathy 63.44 19.84 8 22440 366234 90239765
Drug ineffective 60.15 19.84 162 22286 1384136 89221863
Sinusitis 55.90 19.84 9 22439 343079 90262920
Iridocyclitis 55.54 19.84 24 22424 3637 90602362
Wound 53.99 19.84 6 22442 302974 90303025
Aspartate aminotransferase increased 52.95 19.84 93 22355 102844 90503155
Vomiting 51.85 19.84 353 22095 787940 89818059
Product storage error 50.20 19.84 41 22407 20200 90585799
Disease progression 49.99 19.84 116 22332 156499 90449500
Lipase increased 49.28 19.84 32 22416 11079 90594920
Wheezing 47.11 19.84 3 22445 238077 90367922
Squamous cell carcinoma 47.04 19.84 30 22418 10071 90595928
Ovarian cancer 46.97 19.84 26 22422 6741 90599258
Metastasis 46.54 19.84 25 22423 6112 90599887
Dehydration 46.40 19.84 129 22319 194318 90411681
Helicobacter infection 44.46 19.84 3 22445 226847 90379152
Erythema multiforme 44.11 19.84 31 22417 12215 90593784
Retinal detachment 44.06 19.84 25 22423 6797 90599202
Malignant melanoma 43.36 19.84 31 22417 12545 90593454
Melanoma recurrent 43.18 19.84 10 22438 189 90605810
Metastases to meninges 42.40 19.84 20 22428 3715 90602284
Mobility decreased 42.15 19.84 6 22442 250728 90355271
Haemophagocytic lymphohistiocytosis 41.93 19.84 33 22415 15426 90590573
Weight increased 41.73 19.84 26 22422 417901 90188098
Musculoskeletal stiffness 41.65 19.84 11 22437 296521 90309478
Pneumonitis 41.60 19.84 53 22395 44117 90561882
Rash maculo-papular 41.56 19.84 51 22397 40882 90565117
Second primary malignancy 41.45 19.84 28 22420 10350 90595649
Blood lactate dehydrogenase increased 41.45 19.84 41 22407 25891 90580108
Fatigue 41.13 19.84 451 21997 1153572 89452427
Nasopharyngitis 41.10 19.84 25 22423 407079 90198920
Metastases to lymph nodes 40.73 19.84 29 22419 11660 90594339
Erysipelas 39.97 19.84 26 22422 9026 90596973
Discomfort 38.86 19.84 10 22438 274325 90331674
Impaired healing 38.46 19.84 6 22442 234193 90371806
Detachment of retinal pigment epithelium 38.37 19.84 11 22437 494 90605505
Metastases to liver 37.85 19.84 41 22407 28766 90577233
Sarcoid-like reaction 37.78 19.84 9 22439 193 90605806
Rhabdomyolysis 36.91 19.84 54 22394 51202 90554797
Alanine aminotransferase increased 35.95 19.84 86 22362 118252 90487747
Immune-mediated enterocolitis 35.01 19.84 19 22429 4738 90601261
Metastases to peritoneum 34.55 19.84 18 22430 4137 90601862
Insomnia 34.32 19.84 20 22428 333454 90272545
Vitreous floaters 34.11 19.84 22 22426 7527 90598472
Type 2 diabetes mellitus 33.84 19.84 5 22443 203239 90402760
Neoplasm progression 33.69 19.84 48 22400 44438 90561561
Fall 33.61 19.84 42 22406 481768 90124231
Blood cholesterol increased 32.67 19.84 6 22442 208006 90397993
Injury 32.53 19.84 5 22443 197344 90408655
Systemic inflammatory response syndrome 31.96 19.84 20 22428 6496 90599503
Hypersensitivity 31.33 19.84 40 22408 454637 90151362
Joint swelling 30.98 19.84 48 22400 503252 90102747
Non-small cell lung cancer recurrent 30.60 19.84 7 22441 125 90605874
Intentional product use issue 30.53 19.84 8 22440 216884 90389115
Myalgia 30.40 19.84 104 22344 175021 90430978
Chest pain 30.38 19.84 21 22427 319624 90286375
Palmar-plantar erythrodysaesthesia syndrome 30.22 19.84 36 22412 27987 90578012
Treatment failure 30.19 19.84 19 22429 303909 90302090
Hyperthermia 30.07 19.84 23 22425 10312 90595687
Xerosis 29.99 19.84 12 22436 1499 90604500
Vaccine virus shedding 29.59 19.84 5 22443 15 90605984
Swelling 28.73 19.84 37 22411 419021 90186978
Metastases to abdominal wall 28.33 19.84 7 22441 176 90605823
Sleep disorder 26.58 19.84 8 22440 198022 90407977
Transaminases increased 26.51 19.84 39 22409 37153 90568846
Metastases to spleen 26.50 19.84 7 22441 231 90605768
Retinopathy 25.69 19.84 14 22434 3520 90602479
Serous retinopathy 25.65 19.84 5 22443 39 90605960
Therapy partial responder 24.90 19.84 29 22419 22014 90583985
Product temperature excursion issue 24.48 19.84 9 22439 894 90605105
Panniculitis lobular 24.19 19.84 5 22443 54 90605945
Neutrophilic panniculitis 23.94 19.84 5 22443 57 90605942
Macular oedema 23.91 19.84 15 22433 4894 90601105
Pulmonary embolism 23.86 19.84 79 22369 130741 90475258
Psoriasis 23.77 19.84 4 22444 147750 90458249
Drug intolerance 23.62 19.84 47 22401 447544 90158455
Sepsis 23.10 19.84 97 22351 179717 90426282
Metastases to bone 23.07 19.84 30 22418 25475 90580524
Abdominal discomfort 22.80 19.84 53 22395 477275 90128724
Immune-mediated hepatitis 22.34 19.84 12 22436 2932 90603067
Acute polyneuropathy 21.93 19.84 7 22441 454 90605545
Metastatic neoplasm 21.68 19.84 14 22434 4801 90601198
Leukoderma 21.66 19.84 5 22443 93 90605906
Anxiety 21.58 19.84 27 22421 309745 90296254
Decreased appetite 21.38 19.84 163 22285 376377 90229622
Amylase increased 21.15 19.84 16 22432 7056 90598943
Immune-mediated lung disease 21.14 19.84 10 22438 1870 90604129
Lower respiratory tract infection 20.63 19.84 19 22429 250640 90355359
Ill-defined disorder 20.61 19.84 10 22438 184881 90421118
Myocarditis 20.54 19.84 21 22427 13785 90592214
Hepatotoxicity 20.50 19.84 39 22409 45803 90560196
Blood alkaline phosphatase increased 20.39 19.84 40 22408 48039 90557960
Cholestasis 20.23 19.84 34 22414 36265 90569734
Migraine 20.18 19.84 11 22437 190381 90415618
Tumour haemorrhage 20.11 19.84 10 22438 2084 90603915
Overdose 20.05 19.84 7 22441 157702 90448297
Angular cheilitis 20.04 19.84 8 22440 993 90605006
Hepatic cytolysis 20.02 19.84 31 22417 30885 90575114
Infective glossitis 20.01 19.84 4 22444 36 90605963
Thyroiditis 19.98 19.84 12 22436 3625 90602374
Neoplasm 19.93 19.84 17 22431 8886 90597113

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 1500.29 17.72 1375 20407 392667 42206886
Malignant neoplasm progression 984.41 17.72 638 21144 107762 42491791
Chills 470.90 17.72 387 21395 93679 42505874
Metastases to central nervous system 460.81 17.72 180 21602 10175 42589378
Death 301.46 17.72 708 21074 470477 42129076
Visual impairment 212.30 17.72 176 21606 42937 42556616
Ejection fraction decreased 206.69 17.72 133 21649 21954 42577599
Product use in unapproved indication 177.77 17.72 329 21453 184127 42415426
Rash 176.87 17.72 417 21365 276537 42323016
Blood creatine phosphokinase increased 145.62 17.72 150 21632 48188 42551365
Uveitis 139.86 17.72 76 21706 9182 42590371
Dermatitis acneiform 115.43 17.72 63 21719 7676 42591877
Second primary malignancy 90.37 17.72 58 21724 9517 42590036
Metastases to liver 89.46 17.72 71 21711 16255 42583298
Paronychia 87.54 17.72 43 21739 4212 42595341
Melanoma recurrent 81.96 17.72 19 21763 165 42599388
Metastases to lung 76.51 17.72 56 21726 11368 42588185
Acne 76.18 17.72 60 21722 13584 42585969
Serous retinal detachment 74.19 17.72 25 21757 919 42598634
Skin toxicity 72.74 17.72 44 21738 6505 42593048
Metastases to stomach 71.21 17.72 15 21767 79 42599474
Drug interaction 67.63 17.72 26 21756 266973 42332580
Metastatic malignant melanoma 67.48 17.72 30 21752 2343 42597210
Fatigue 62.57 17.72 408 21374 435233 42164320
Vision blurred 59.48 17.72 102 21680 53597 42545956
Chorioretinopathy 58.96 17.72 24 21758 1507 42598046
Malignant melanoma 58.29 17.72 44 21738 9356 42590197
Metastases to lymph nodes 58.25 17.72 37 21745 5961 42593592
Hyperpyrexia 56.08 17.72 30 21752 3510 42596043
Blood lactate dehydrogenase increased 54.58 17.72 67 21715 26014 42573539
Product storage error 53.76 17.72 45 21737 11095 42588458
Toxicity to various agents 53.69 17.72 25 21757 229111 42370442
C-reactive protein increased 50.80 17.72 105 21677 63455 42536098
Haemophagocytic lymphohistiocytosis 50.27 17.72 54 21728 18168 42581385
Metastases to peritoneum 48.15 17.72 24 21758 2425 42597128
Metastases to meninges 46.97 17.72 22 21760 1939 42597614
Intestinal metastasis 46.91 17.72 14 21768 344 42599209
Metastases to bone 46.44 17.72 47 21735 14762 42584791
Malignant mesenteric neoplasm 43.81 17.72 9 21773 41 42599512
Febrile neutropenia 39.42 17.72 23 21759 185680 42413873
Nausea 38.93 17.72 340 21442 396459 42203094
Anxiety 36.46 17.72 8 21774 118552 42481001
Metastasis 35.95 17.72 25 21757 4680 42594873
Detachment of retinal pigment epithelium 35.81 17.72 13 21769 597 42598956
Condition aggravated 35.40 17.72 49 21733 260705 42338848
Procalcitonin increased 35.24 17.72 19 21763 2257 42597296
Product temperature excursion issue 34.78 17.72 12 21770 474 42599079
Vomiting 34.74 17.72 260 21522 289463 42310090
Overdose 34.69 17.72 6 21776 105258 42494295
Anaplastic thyroid cancer 33.60 17.72 6 21776 10 42599543
Squamous cell carcinoma 33.25 17.72 37 21745 12945 42586608
BRAF V600E mutation positive 33.21 17.72 7 21775 37 42599516
Erythema nodosum 33.09 17.72 17 21765 1831 42597722
Metastases to skin 32.96 17.72 12 21770 556 42598997
Dermatitis 32.41 17.72 35 21747 11840 42587713
Vogt-Koyanagi-Harada disease 31.41 17.72 9 21773 191 42599362
Panniculitis 30.44 17.72 17 21765 2164 42597389
Decreased appetite 30.10 17.72 185 21597 192952 42406601
Dehydration 29.59 17.72 147 21635 141620 42457933
Retinal detachment 28.71 17.72 25 21757 6500 42593053
Concomitant disease aggravated 28.51 17.72 25 21757 6561 42592992
Mesenteric neoplasm 28.42 17.72 6 21776 32 42599521
Metastases to heart 28.41 17.72 8 21774 159 42599394
Jejunal ulcer perforation 28.30 17.72 7 21775 82 42599471
Left ventricular dysfunction 28.12 17.72 32 21750 11469 42588084
Brain neoplasm 27.36 17.72 19 21763 3549 42596004
Drug ineffective 26.65 17.72 201 21581 629996 41969557
Depression 26.28 17.72 12 21770 111351 42488202
Basal cell carcinoma 26.23 17.72 44 21738 22689 42576864
Therapy partial responder 26.16 17.72 41 21741 19980 42579573
Dry skin 24.59 17.72 67 21715 48271 42551282
Ureteral disorder 24.10 17.72 7 21775 156 42599397
Omental necrosis 23.95 17.72 5 21777 25 42599528
Eastern Cooperative Oncology Group performance status 23.04 17.72 5 21777 31 42599522
Blood alkaline phosphatase increased 22.82 17.72 52 21730 33545 42566008
Chronic obstructive pulmonary disease 22.15 17.72 3 21779 63111 42536442
Gastrointestinal wall thickening 22.09 17.72 13 21769 1826 42597727
Acute polyneuropathy 22.06 17.72 7 21775 212 42599341
Tumour invasion 21.98 17.72 8 21774 370 42599183
Retinopathy 21.97 17.72 14 21768 2267 42597286
General physical health deterioration 21.76 17.72 142 21640 151104 42448449
Myocardial infarction 21.53 17.72 19 21763 123990 42475563
Pneumonitis 21.40 17.72 58 21724 41660 42557893
Therapeutic product effect incomplete 21.37 17.72 5 21777 70934 42528619
Disease progression 21.35 17.72 136 21646 143520 42456033
Varicella virus test positive 21.29 17.72 7 21775 238 42599315
Hyperthermia 21.14 17.72 29 21753 12545 42587008
Neurofibrosarcoma 20.85 17.72 5 21777 51 42599502
Cerebral haemorrhage 20.82 17.72 55 21727 38911 42560642
BRAF gene mutation 20.42 17.72 5 21777 56 42599497
Folliculitis 19.96 17.72 19 21763 5539 42594014
Iridocyclitis 19.89 17.72 13 21769 2198 42597355
Abdominal lymphadenopathy 19.80 17.72 10 21772 1039 42598514
Blood pressure increased 19.73 17.72 14 21768 101914 42497639
Papilloedema 19.53 17.72 15 21767 3271 42596282
Fat necrosis 19.50 17.72 7 21775 311 42599242
Aspartate aminotransferase increased 19.00 17.72 84 21698 77079 42522474
Asthenia 18.95 17.72 223 21559 280570 42318983
Lymphadenopathy 18.75 17.72 48 21734 33317 42566236
Leukoderma 18.22 17.72 5 21777 90 42599463
Influenza like illness 18.10 17.72 46 21736 31794 42567759
Brain neoplasm malignant 17.85 17.72 9 21773 932 42598621
Coronary artery disease 17.83 17.72 3 21779 53717 42545836

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 2246.95 18.21 1974 31664 896291 109659370
Malignant neoplasm progression 1934.29 18.21 977 32661 173590 110382071
Metastases to central nervous system 572.35 18.21 227 33411 22590 110533071
Chills 557.36 18.21 462 33176 190118 110365543
Death 505.14 18.21 820 32818 698049 109857612
Ejection fraction decreased 385.32 18.21 206 33432 40674 110514987
Uveitis 328.50 18.21 151 33487 21559 110534102
Blood creatine phosphokinase increased 293.41 18.21 214 33424 72863 110482798
Dermatitis acneiform 275.95 18.21 114 33524 12581 110543080
Paronychia 189.59 18.21 84 33554 10997 110544664
Product use in unapproved indication 189.50 18.21 419 33219 446958 110108703
Rash 177.53 18.21 600 33038 820364 109735297
Skin toxicity 169.01 18.21 79 33559 11704 110543957
Panniculitis 156.59 18.21 82 33556 15500 110540161
Serous retinal detachment 152.79 18.21 44 33594 1628 110554033
Metastatic malignant melanoma 133.32 18.21 47 33591 3362 110552299
Chorioretinopathy 130.80 18.21 42 33596 2253 110553408
Metastases to lung 129.18 18.21 83 33555 22980 110532681
Hyperpyrexia 124.77 18.21 57 33581 8012 110547649
Metastases to liver 116.26 18.21 92 33546 35294 110520367
Blood lactate dehydrogenase increased 111.95 18.21 99 33539 44235 110511426
Erythema nodosum 109.22 18.21 49 33589 6604 110549057
BRAF V600E mutation positive 105.98 18.21 19 33619 68 110555593
Melanoma recurrent 102.03 18.21 23 33615 308 110555353
Haemophagocytic lymphohistiocytosis 101.43 18.21 81 33557 31478 110524183
Second primary malignancy 101.13 18.21 65 33573 18003 110537658
Squamous cell carcinoma 97.40 18.21 64 33574 18399 110537262
Visual impairment 93.97 18.21 156 33482 134272 110421389
Metastases to lymph nodes 93.96 18.21 58 33580 14974 110540687
Drug hypersensitivity 87.85 18.21 16 33622 454074 110101587
Vogt-Koyanagi-Harada disease 87.83 18.21 23 33615 593 110555068
Malignant melanoma 85.35 18.21 57 33581 16834 110538827
Condition aggravated 85.01 18.21 60 33578 734776 109820885
Aspartate aminotransferase increased 81.72 18.21 162 33476 159774 110395887
Metastases to peritoneum 81.65 18.21 38 33600 5572 110550089
Detachment of retinal pigment epithelium 81.03 18.21 24 33614 981 110554680
Metastasis 75.99 18.21 41 33597 8226 110547435
Dehydration 72.56 18.21 218 33420 279293 110276368
Rheumatoid arthritis 71.73 18.21 5 33633 299608 110256053
Metastases to bone 71.23 18.21 66 33572 31306 110524355
Iridocyclitis 70.64 18.21 34 33604 5374 110550287
Vision blurred 69.93 18.21 134 33504 128888 110426773
Retinal detachment 69.81 18.21 43 33595 11057 110544604
Metastases to meninges 69.29 18.21 33 33605 5095 110550566
Procalcitonin increased 60.67 18.21 28 33610 4028 110551633
Sinusitis 60.59 18.21 9 33629 296679 110258982
Pneumonitis 60.56 18.21 94 33544 76437 110479224
Lipase increased 60.16 18.21 48 33590 18624 110537037
Disease progression 56.53 18.21 183 33455 243851 110311810
Wheezing 56.35 18.21 6 33632 255224 110300437
Vomiting 56.06 18.21 470 33168 910205 109645456
Metastases to stomach 55.93 18.21 14 33624 300 110555361
Alanine aminotransferase increased 55.09 18.21 151 33487 183622 110372039
Joint swelling 54.04 18.21 34 33604 442811 110112850
Arthropathy 53.74 18.21 11 33627 287511 110268150
Drug interaction 52.50 18.21 45 33593 500138 110055523
Blood alkaline phosphatase increased 51.81 18.21 84 33554 70851 110484810
Rash maculo-papular 50.32 18.21 85 33553 74137 110481524
Nasopharyngitis 49.90 18.21 29 33609 394332 110161329
Musculoskeletal stiffness 49.68 18.21 12 33626 279810 110275851
Mobility decreased 48.94 18.21 7 33631 237415 110318246
Therapy partial responder 48.31 18.21 58 33580 37003 110518658
C-reactive protein increased 48.30 18.21 161 33477 217758 110337903
Psoriatic arthropathy 47.92 18.21 3 33635 196758 110358903
Drug ineffective 47.74 18.21 270 33368 1520270 109035391
Therapeutic product effect incomplete 47.56 18.21 6 33632 223799 110331862
Weight increased 47.49 18.21 35 33603 419609 110136052
Anxiety 47.15 18.21 23 33615 345055 110210606
Malignant mesenteric neoplasm 46.53 18.21 9 33629 53 110555608
BRAF gene mutation 45.70 18.21 9 33629 59 110555602
Hyperthermia 44.93 18.21 43 33595 21229 110534432
Toxicity to various agents 43.76 18.21 49 33589 480506 110075155
Helicobacter infection 43.62 18.21 3 33635 181874 110373787
Overdose 43.57 18.21 9 33629 233785 110321876
Acute polyneuropathy 43.54 18.21 14 33624 754 110554907
Erysipelas 42.76 18.21 34 33604 13124 110542537
Decreased appetite 42.69 18.21 269 33369 475577 110080084
Metastases to skin 41.17 18.21 18 33620 2281 110553380
Dry skin 41.15 18.21 97 33541 107556 110448105
Sarcoid-like reaction 40.90 18.21 11 33627 315 110555346
Retinopathy 40.80 18.21 22 33616 4407 110551254
Intestinal metastasis 39.47 18.21 12 33626 537 110555124
Rhabdomyolysis 39.17 18.21 102 33536 120299 110435362
Osteoarthritis 38.55 18.21 5 33633 182618 110373043
Insomnia 38.35 18.21 32 33606 360558 110195103
Acne 38.14 18.21 49 33589 33471 110522190
Visual acuity reduced 38.14 18.21 48 33590 32125 110523536
Hypersensitivity 38.09 18.21 40 33598 403958 110151703
Serous retinopathy 37.92 18.21 10 33628 265 110555396
Amylase increased 37.82 18.21 31 33607 12488 110543173
Product dose omission issue 37.49 18.21 26 33612 321756 110233905
Type 2 diabetes mellitus 37.06 18.21 5 33633 177227 110378434
Dermatitis 37.00 18.21 44 33594 27793 110527868
Blood cholesterol increased 36.82 18.21 6 33632 184779 110370882
Nausea 36.48 18.21 552 33086 1235138 109320523
Diarrhoea 36.37 18.21 516 33122 1138989 109416672
Swelling 36.30 18.21 32 33606 351009 110204652
Gamma-glutamyltransferase increased 36.10 18.21 66 33572 61243 110494418
Lymphadenopathy 35.43 18.21 67 33571 63768 110491893
Acquired gene mutation 35.02 18.21 17 33621 2737 110552924
Basal cell carcinoma 34.96 18.21 55 33583 45215 110510446
Injury 34.78 18.21 6 33632 177259 110378402
Intentional product use issue 34.65 18.21 16 33622 247890 110307771
Impaired healing 33.83 18.21 9 33629 196708 110358953
Metastases to adrenals 33.49 18.21 14 33624 1589 110554072
Discomfort 33.02 18.21 12 33626 214695 110340966
Metastatic neoplasm 32.54 18.21 21 33617 5852 110549809
Concomitant disease aggravated 32.54 18.21 32 33606 16332 110539329
Abdominal lymphadenopathy 31.72 18.21 14 33624 1814 110553847
Chest pain 31.46 18.21 41 33597 376334 110179327
Wound 31.44 18.21 16 33622 234421 110321240
Erythema multiforme 30.80 18.21 35 33603 21062 110534599
Tumour invasion 30.54 18.21 10 33628 571 110555090
Fall 30.27 18.21 89 33549 603393 109952268
Treatment failure 30.22 18.21 24 33614 277210 110278451
Pain 30.16 18.21 169 33469 954786 109600875
Xerosis 29.82 18.21 13 33625 1636 110554025
Intentional overdose 29.53 18.21 3 33635 132498 110423163
Jejunal ulcer perforation 29.49 18.21 7 33631 119 110555542
Left ventricular dysfunction 29.37 18.21 36 33602 23457 110532204
Demyelinating polyneuropathy 28.95 18.21 14 33624 2235 110553426
Cerebral haemorrhage 28.68 18.21 62 33576 64906 110490755
Therapy cessation 28.60 18.21 50 33588 44807 110510854
Hepatotoxicity 28.56 18.21 61 33577 63339 110492322
Depression 28.17 18.21 33 33605 317302 110238359
Intestinal perforation 27.66 18.21 33 33605 20911 110534750
Drug intolerance 27.56 18.21 51 33587 406461 110149200
Blood pressure increased 27.37 18.21 23 33615 258350 110297311
Rash pustular 27.22 18.21 26 33612 12803 110542858
Peritoneal disorder 27.09 18.21 10 33628 816 110554845
Cutaneous sarcoidosis 26.77 18.21 9 33629 558 110555103
Hypophysitis 26.70 18.21 18 33620 5397 110550264
Sleep disorder 25.98 18.21 14 33624 198630 110357031
Non-small cell lung cancer recurrent 25.94 18.21 7 33631 203 110555458
Brain oedema 25.72 18.21 39 33599 31059 110524602
Migraine 25.71 18.21 10 33628 171642 110384019
Blister 25.65 18.21 19 33619 227357 110328304
Fatigue 25.33 18.21 514 33124 1215444 109340217
Mesenteric neoplasm 25.17 18.21 6 33632 104 110555557
Intentional product misuse 24.99 18.21 5 33633 132899 110422762
Hypoalbuminaemia 24.91 18.21 37 33601 28937 110526724
Tumour haemorrhage 24.82 18.21 17 33621 5228 110550433
Macular oedema 24.80 18.21 19 33619 6947 110548714
COVID-19 24.54 18.21 23 33615 245037 110310624
Omental necrosis 24.52 18.21 5 33633 40 110555621
Contusion 24.44 18.21 21 33617 233340 110322321
Hepatic function abnormal 24.41 18.21 71 33567 89224 110466437
Obesity 24.17 18.21 3 33635 113348 110442313
Transaminases increased 24.09 18.21 57 33581 63333 110492328
Metastases to pleura 24.04 18.21 12 33626 2051 110553610
Papilloedema 23.76 18.21 19 33619 7390 110548271
Embolism 23.74 18.21 27 33611 16262 110539399
Metastases to spleen 23.27 18.21 9 33629 835 110554826
Influenza like illness 22.94 18.21 69 33569 88343 110467318
Ureteral disorder 22.52 18.21 8 33630 585 110555076
Disseminated intravascular coagulation 22.50 18.21 43 33595 41243 110514418
Vitreous floaters 22.26 18.21 20 33618 9114 110546547
Panniculitis lobular 22.25 18.21 5 33633 66 110555595
Hepatitis 22.16 18.21 69 33569 89985 110465676
Hyperkeratosis 22.06 18.21 20 33618 9219 110546442
Abdominal discomfort 22.05 18.21 55 33583 393803 110161858
Gastrooesophageal reflux disease 21.68 18.21 14 33624 179962 110375699
Autoimmune colitis 21.53 18.21 11 33627 1974 110553687
Varicella virus test positive 21.46 18.21 7 33631 395 110555266
Ingrowing nail 21.44 18.21 13 33625 3249 110552412
Thyroiditis 21.39 18.21 17 33621 6556 110549105
Neoplasm progression 21.28 18.21 55 33583 64540 110491121
Psoriasis 21.22 18.21 8 33630 139985 110415676
Metastases to heart 20.96 18.21 7 33631 425 110555236
Squamous cell carcinoma of skin 20.92 18.21 26 33612 17177 110538484
Hepatocellular injury 20.85 18.21 47 33591 50595 110505066
Lower respiratory tract infection 20.80 18.21 26 33612 243080 110312581
Hypoaesthesia 20.78 18.21 40 33598 314183 110241478
Adverse event 20.66 18.21 4 33634 108805 110446856
Ill-defined disorder 20.59 18.21 11 33627 156842 110398819
Asthenia 20.31 18.21 308 33330 688691 109866970
Pancreatic enzymes increased 19.98 18.21 10 33628 1719 110553942
Vitiligo 19.77 18.21 12 33626 3005 110552656
Musculoskeletal pain 19.74 18.21 16 33622 183007 110372654
Photosensitivity reaction 19.63 18.21 31 33607 25558 110530103
Febrile neutropenia 19.52 18.21 42 33596 316725 110238936
Myalgia 19.45 18.21 125 33513 222256 110333405
Metastases to thorax 19.41 18.21 6 33632 284 110555377
Eczema 19.30 18.21 57 33581 72236 110483425
Suicide attempt 19.21 18.21 4 33634 103390 110452271
Brain neoplasm malignant 19.19 18.21 10 33628 1870 110553791
Urticaria 19.06 18.21 43 33595 318814 110236847
Malignant melanoma stage IV 18.98 18.21 5 33633 132 110555529
Drug resistance 18.57 18.21 48 33590 56326 110499335
Eastern Cooperative Oncology Group performance status 18.56 18.21 5 33633 144 110555517
Nodular rash 18.54 18.21 6 33632 330 110555331
Paraesthesia 18.46 18.21 35 33603 276486 110279175
Cholestasis 18.31 18.21 52 33586 64466 110491195

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 agent
CHEBI has role CHEBI:79091 EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
CHEBI has role CHEBI:149553 anticoronaviral agent
CHEBI has role CHEBI:176497 geroprotector

Related Drugs by ATC class:

L01EE Mitogen-activated protein kinase (MEK) inhibitors 4 drugs
binimetinibcobimetinibmirdametinibselumetinib

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 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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 Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 1MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
EQ 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL Sept. 16, 2026 PEDIATRIC EXCLUSIVITY
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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY
EQ 1MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY
EQ 0.05MG BASE/ML MEKINIST NOVARTIS N217513 March 16, 2023 RX SOLUTION ORAL Sept. 16, 2030 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Dual specificity mitogen-activated protein kinase kinase 1 Kinase INHIBITOR IC50 8.75 WOMBAT-PK CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase INHIBITOR IC50 9.04 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
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
9421 INN_ID
11707110 PUBCHEM_CID
33E86K87QN INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 0078-1161 POWDER, FOR SOLUTION 0.05 mg ORAL NDA 32 sections