trametinib 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: 4.84
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 102.06
  • ALOGS: -4.30
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

None

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

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 2213.25 40.60 645 2154 53063 2302223
Malignant neoplasm progression 783.58 40.60 211 2588 11917 2343369
Chills 607.87 40.60 183 2616 15369 2339917
Rash 454.98 40.60 211 2588 59347 2295939
Death 386.56 40.60 209 2590 81259 2274027
Nausea 309.44 40.60 203 2596 111986 2243300
Diarrhoea 292.15 40.60 176 2623 83388 2271898
Vomiting 247.63 40.60 150 2649 71452 2283834
Fatigue 231.51 40.60 153 2646 84720 2270566
Panniculitis 230.10 40.60 44 2755 491 2354795
Metastatic malignant melanoma 204.89 40.60 37 2762 293 2354993
Uveitis 192.25 40.60 46 2753 1559 2353727
Product use in unapproved indication 191.32 40.60 71 2728 11129 2344157
Dehydration 181.11 40.60 83 2716 22212 2333074
Visual impairment 173.56 40.60 67 2732 11688 2343598
Ejection fraction decreased 171.46 40.60 47 2752 2754 2352532
Metastases to central nervous system 169.20 40.60 44 2755 2104 2353182
Malignant melanoma 167.58 40.60 43 2756 1949 2353337
Blood creatine phosphokinase increased 135.31 40.60 45 2754 5091 2350195
Dermatitis acneiform 132.99 40.60 30 2769 779 2354507
Decreased appetite 124.14 40.60 70 2729 28821 2326465
Neutropenia 119.88 40.60 62 2737 21486 2333800
Arthralgia 112.34 40.60 83 2716 54202 2301084
Hypotension 106.31 40.60 66 2733 32370 2322916
Malignant melanoma stage IV 103.10 40.60 15 2784 20 2355266
Sepsis 102.22 40.60 53 2746 18435 2336851
Aspartate aminotransferase increased 99.19 40.60 46 2753 12566 2342720
Vision blurred 98.56 40.60 48 2751 14620 2340666
Headache 95.54 40.60 89 2710 80090 2275196
General physical health deterioration 94.18 40.60 46 2753 14093 2341193
Alanine aminotransferase increased 91.51 40.60 45 2754 13987 2341299
C-reactive protein increased 89.85 40.60 35 2764 6220 2349066
Anaemia 85.15 40.60 59 2740 34733 2320553
Product use issue 82.25 40.60 40 2759 12129 2343157
Urinary tract infection 80.92 40.60 54 2745 29888 2325398
Chorioretinopathy 78.78 40.60 16 2783 247 2355039
Abdominal pain 76.46 40.60 55 2744 34319 2320967
Infection 75.44 40.60 43 2756 17986 2337300
Pneumonia 73.03 40.60 62 2737 49234 2306052
Pulmonary embolism 72.64 40.60 42 2757 18041 2337245
Rhabdomyolysis 70.50 40.60 30 2769 6674 2348612
Paronychia 70.33 40.60 18 2781 804 2354482
Disease progression 66.79 40.60 39 2760 17056 2338230
Seizure 65.75 40.60 44 2755 24422 2330864
Peripheral swelling 65.74 40.60 39 2760 17558 2337728
Myalgia 65.21 40.60 43 2756 23290 2331996
Cough 64.65 40.60 49 2750 33068 2322218
Dry skin 64.14 40.60 28 2771 6624 2348662
Oedema peripheral 62.09 40.60 42 2757 23721 2331565
Rash maculo-papular 61.77 40.60 24 2775 4228 2351058
Thrombocytopenia 60.21 40.60 38 2761 19093 2336193
Hepatic enzyme increased 59.61 40.60 30 2769 9772 2345514
Asthenia 59.39 40.60 54 2745 46872 2308414
Pancreatitis 58.93 40.60 28 2771 8051 2347235
Constipation 58.35 40.60 39 2760 21590 2333696
Erythema 57.59 40.60 41 2758 25118 2330168
Malaise 57.11 40.60 57 2742 55528 2299758
Systemic inflammatory response syndrome 56.65 40.60 15 2784 766 2354520
Confusional state 56.48 40.60 40 2759 24304 2330982
Erythema nodosum 56.29 40.60 15 2784 785 2354501
Pneumonitis 55.85 40.60 22 2777 4017 2351269
Retinal detachment 55.19 40.60 16 2783 1143 2354143
Hyponatraemia 53.61 40.60 31 2768 13294 2341992
Influenza like illness 50.92 40.60 29 2770 12085 2343201
Hyperpyrexia 50.62 40.60 13 2786 588 2354698
Liver function test increased 50.40 40.60 19 2780 3082 2352204
Colitis 50.38 40.60 22 2777 5204 2350082
Pyelonephritis 49.39 40.60 17 2782 2124 2353162
Hypokalaemia 48.83 40.60 27 2772 10627 2344659
Dizziness 47.49 40.60 53 2746 58612 2296674
Blood lactate dehydrogenase increased 44.76 40.60 18 2781 3466 2351820
Hypoalbuminaemia 43.90 40.60 14 2785 1380 2353906
Abdominal pain upper 43.73 40.60 33 2766 22067 2333219
Pain 43.53 40.60 52 2747 61805 2293481
Cellulitis 41.29 40.60 23 2776 9178 2346108
Metastases to lung 40.92 40.60 14 2785 1717 2353569
Metastasis 40.64 40.60 12 2787 914 2354372

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 1936.79 38.15 641 2289 45759 1698092
Malignant neoplasm progression 823.19 38.15 256 2674 13902 1729949
Chills 584.77 38.15 189 2741 11498 1732353
Death 465.86 38.15 292 2638 87151 1656700
Metastatic malignant melanoma 380.32 38.15 71 2859 370 1743481
Metastases to central nervous system 343.44 38.15 81 2849 1464 1742387
Rash 317.04 38.15 172 2758 38521 1705330
Ejection fraction decreased 279.56 38.15 74 2856 2171 1741680
Fatigue 245.99 38.15 161 2769 50620 1693231
Malignant melanoma 199.87 38.15 53 2877 1560 1742291
Nausea 187.77 38.15 137 2793 51059 1692792
Diarrhoea 177.10 38.15 135 2795 53717 1690134
Vomiting 164.41 38.15 113 2817 38202 1705649
Dehydration 153.37 38.15 82 2848 17576 1726275
Product use in unapproved indication 139.47 38.15 63 2867 9359 1734492
Decreased appetite 137.98 38.15 85 2845 23786 1720065
Visual impairment 136.52 38.15 55 2875 6163 1737688
Blood creatine phosphokinase increased 124.05 38.15 57 2873 8799 1735052
C-reactive protein increased 115.32 38.15 48 2882 5837 1738014
Uveitis 108.83 38.15 30 2900 1021 1742830
Disease progression 95.84 38.15 60 2870 17203 1726648
General physical health deterioration 94.67 38.15 54 2876 13064 1730787
Malignant melanoma stage IV 94.04 38.15 15 2915 22 1743829
Vision blurred 92.83 38.15 46 2884 8377 1735474
Metastases to liver 89.98 38.15 31 2899 2236 1741615
Asthenia 88.03 38.15 75 2855 34595 1709256
Basal cell carcinoma 83.44 38.15 30 2900 2453 1741398
Dermatitis acneiform 73.02 38.15 22 2908 1030 1742821
Acne 72.82 38.15 25 2905 1783 1742068
Squamous cell carcinoma 71.98 38.15 25 2905 1846 1742005
Metastases to bone 69.87 38.15 24 2906 1714 1742137
Second primary malignancy 68.59 38.15 21 2909 1038 1742813
Chorioretinopathy 68.35 38.15 17 2913 383 1743468
Headache 66.75 38.15 64 2866 34312 1709539
Confusional state 64.29 38.15 51 2879 21227 1722624
Arthralgia 64.09 38.15 53 2877 23391 1720460
Abdominal pain 63.84 38.15 51 2879 21439 1722412
Pneumonitis 63.64 38.15 28 2902 3887 1739964
Pneumonia 59.36 38.15 69 2861 46113 1697738
Metastases to meninges 58.00 38.15 14 2916 277 1743574
Thrombocytopenia 57.98 38.15 48 2882 21201 1722650
Neutropenia 57.79 38.15 45 2885 18215 1725636
Anaemia 57.44 38.15 55 2875 29402 1714449
Hypotension 57.12 38.15 55 2875 29599 1714252
Atrial fibrillation 56.15 38.15 41 2889 15070 1728781
Sepsis 53.21 38.15 44 2886 19394 1724457
Metastases to skin 53.00 38.15 11 2919 105 1743746
Hyponatraemia 51.65 38.15 32 2898 8968 1734883
Cough 51.60 38.15 43 2887 19154 1724697
Metastases to lymph nodes 51.13 38.15 16 2914 850 1743001
Product use issue 50.52 38.15 31 2899 8540 1735311
Liver function test increased 49.46 38.15 18 2912 1521 1742330
Squamous cell carcinoma of skin 49.32 38.15 17 2913 1225 1742626
Panniculitis 48.37 38.15 11 2919 166 1743685
Acute kidney injury 47.85 38.15 54 2876 34890 1708961
Alanine aminotransferase increased 47.15 38.15 34 2896 12244 1731607
Hepatic enzyme increased 46.99 38.15 27 2903 6594 1737257
Malaise 46.22 38.15 49 2881 29516 1714335
Rash maculo-papular 46.08 38.15 22 2908 3681 1740170
Metastases to lung 45.80 38.15 17 2913 1518 1742333
Leukopenia 45.76 38.15 29 2901 8451 1735400
Peripheral swelling 44.87 38.15 28 2902 7943 1735908
Aspartate aminotransferase increased 44.10 38.15 31 2899 10725 1733126
Night sweats 42.62 38.15 18 2912 2258 1741593
Blood alkaline phosphatase increased 41.78 38.15 23 2907 5172 1738679
Epilepsy 41.72 38.15 21 2909 3938 1739913
Concomitant disease aggravated 40.67 38.15 13 2917 740 1743111
Infection 40.24 38.15 31 2899 12329 1731522
Blood lactate dehydrogenase increased 40.21 38.15 20 2910 3655 1740196
Rhabdomyolysis 38.71 38.15 29 2901 11061 1732790
Influenza like illness 38.51 38.15 23 2907 6030 1737821
Papilloedema 38.50 38.15 12 2918 629 1743222

Pharmacologic Action:

SourceCodeDescription
ATC L01XE25 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
FDA EPC N0000175605 Kinase Inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastatic malignant melanoma indication 443493003
Malignant Melanoma with BRAF V600K Mutation indication
Malignant Melanoma with BRAF V600E Mutation indication

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 0.5MG 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

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 May 29, 2020 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 May 29, 2020 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 May 29, 2020 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 June 22, 2020 MEKINIST, 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 June 22, 2020 MEKINIST, 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 June 22, 2020 MEKINIST, 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 Jan. 8, 2021 TRAMETINIB IN COMBO WITH DABRAFENIB FOR TX. OF PTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST. THIS INDICATION IS BASED ON THE DEMONSTRATION OF DURABLE RESPONSE RATE
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Jan. 8, 2021 TRAMETINIB IN COMBO WITH DABRAFENIB FOR TX. OF PTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST. THIS INDICATION IS BASED ON THE DEMONSTRATION OF DURABLE RESPONSE RATE
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Jan. 8, 2021 TRAMETINIB IN COMBO WITH DABRAFENIB FOR TX. OF PTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST. THIS INDICATION IS BASED ON THE DEMONSTRATION OF DURABLE RESPONSE RATE
EQ 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL April 30, 2021 DABRAFENIB 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL April 30, 2021 DABRAFENIB 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL April 30, 2021 DABRAFENIB 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL May 4, 2021 DABRAFENIB 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 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL May 4, 2021 DABRAFENIB 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 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL May 4, 2021 DABRAFENIB 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 0.5MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Oct. 6, 2022 ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 1MG MEKINIST NOVARTIS N204114 May 29, 2013 DISCN TABLET ORAL Oct. 6, 2022 ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 2MG MEKINIST NOVARTIS N204114 May 29, 2013 RX TABLET ORAL Oct. 6, 2022 ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 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 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

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 8.74 WOMBAT-PK CHEMBL

External reference:

IDSource
D10175 KEGG_DRUG
C3644500 UMLSCUI
33E86K87QN UNII
9421 INN_ID
1187431-43-1 SECONDARY_CAS_RN
DB08911 DRUGBANK_ID
CHEBI:75998 CHEBI
C560077 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2103875 ChEMBL_ID
CHEMBL2105741 ChEMBL_ID
11707110 PUBCHEM_CID
6495 IUPHAR_LIGAND_ID
715545006 SNOMEDCT_US
1425099 RXNORM
29478 MMSL
d08104 MMSL
015044 NDDF
4032511 VANDF
708711009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0666 TABLET, FILM COATED 0.50 mg ORAL NDA 18 sections
Mekinist HUMAN PRESCRIPTION DRUG LABEL 1 0078-0668 TABLET, FILM COATED 2 mg ORAL NDA 18 sections