dabrafenib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors 4801 1195765-45-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • GSK2118436B
  • dabrafenib mesylate
  • tafinlar
  • dabrafenib
  • GSK2118436
  • dabrafenib mesilate
Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.
  • Molecular weight: 519.56
  • Formula: C23H20F3N5O2S2
  • CLOGP: 4.61
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 2
  • TPSA: 110.86
  • ALOGS: -5.20
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 0.65 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.86 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 26, 2013 EMA Novartis Europharm Limited
May 29, 2013 FDA NOVARTIS PHARMS CORP

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 2317.13 42.54 656 1948 53052 2302429
Malignant neoplasm progression 746.58 42.54 200 2404 11928 2343553
Chills 639.10 42.54 187 2417 15365 2340116
Death 378.28 42.54 201 2403 81267 2274214
Rash 336.46 42.54 168 2436 59390 2296091
Nausea 308.19 42.54 197 2407 111992 2243489
Vomiting 260.63 42.54 151 2453 71451 2284030
Metastatic malignant melanoma 247.74 42.54 43 2561 287 2355194
Fatigue 246.98 42.54 155 2449 84718 2270763
Panniculitis 239.62 42.54 45 2559 490 2354991
Diarrhoea 239.03 42.54 151 2453 83413 2272068
Metastases to central nervous system 217.52 42.54 53 2551 2095 2353386
Uveitis 211.45 42.54 49 2555 1556 2353925
Malignant melanoma 200.92 42.54 49 2555 1943 2353538
Dehydration 170.97 42.54 78 2526 22217 2333264
Visual impairment 156.72 42.54 61 2543 11694 2343787
Arthralgia 151.67 42.54 97 2507 54188 2301293
Ejection fraction decreased 142.37 42.54 40 2564 2761 2352720
Headache 128.32 42.54 102 2502 80077 2275404
Decreased appetite 126.15 42.54 69 2535 28822 2326659
General physical health deterioration 122.67 42.54 54 2550 14085 2341396
Neutropenia 115.36 42.54 59 2545 21489 2333992
Blood creatine phosphokinase increased 106.74 42.54 37 2567 5099 2350382
Malignant melanoma stage IV 104.19 42.54 15 2589 20 2355461
Myalgia 96.99 42.54 54 2550 23279 2332202
Vision blurred 95.76 42.54 46 2558 14622 2340859
C-reactive protein increased 92.32 42.54 35 2569 6220 2349261
Product use in unapproved indication 88.19 42.54 40 2564 11160 2344321
Hypotension 87.88 42.54 57 2547 32379 2323102
Dermatitis acneiform 87.12 42.54 21 2583 788 2354693
Aspartate aminotransferase increased 83.66 42.54 40 2564 12572 2342909
Alanine aminotransferase increased 82.56 42.54 41 2563 13991 2341490
Sepsis 80.11 42.54 44 2560 18444 2337037
Asthenia 77.52 42.54 61 2543 46865 2308616
Infection 72.88 42.54 41 2563 17988 2337493
Pulmonary embolism 72.77 42.54 41 2563 18042 2337439
Rash maculo-papular 70.79 42.54 26 2578 4226 2351255
Disease progression 69.43 42.54 39 2565 17056 2338425
Anaemia 67.92 42.54 50 2554 34742 2320739
Basal cell carcinoma 66.16 42.54 22 2582 2665 2352816
Rhabdomyolysis 65.89 42.54 28 2576 6676 2348805
Cough 65.56 42.54 48 2556 33069 2322412
Urinary tract infection 62.91 42.54 45 2559 29897 2325584
Erythema nodosum 62.22 42.54 16 2588 784 2354697
Confusional state 61.52 42.54 41 2563 24303 2331178
Peripheral swelling 57.82 42.54 35 2569 17562 2337919
Hyperkeratosis 57.12 42.54 15 2589 798 2354683
Chorioretinopathy 56.50 42.54 12 2592 251 2355230
Constipation 56.02 42.54 37 2567 21592 2333889
Hyponatraemia 55.71 42.54 31 2573 13294 2342187
Erythema 55.57 42.54 39 2565 25120 2330361
Product use issue 55.54 42.54 30 2574 12139 2343342
Abdominal pain 55.20 42.54 44 2560 34330 2321151
Pneumonia 54.60 42.54 51 2553 49245 2306236
Seizure 54.21 42.54 38 2566 24428 2331053
Malaise 53.08 42.54 53 2551 55532 2299949
Systemic inflammatory response syndrome 52.91 42.54 14 2590 767 2354714
Influenza like illness 52.88 42.54 29 2575 12085 2343396
Hepatic enzyme increased 52.79 42.54 27 2577 9775 2345706
Thrombocytopenia 52.64 42.54 34 2570 19097 2336384
Dizziness 52.49 42.54 54 2550 58611 2296870
Retinal detachment 51.86 42.54 15 2589 1144 2354337
Liver function test increased 51.74 42.54 19 2585 3082 2352399
Hyperpyrexia 51.56 42.54 13 2591 588 2354893
Metastasis 50.55 42.54 14 2590 912 2354569
Metastases to lung 50.01 42.54 16 2588 1715 2353766
Dry skin 46.82 42.54 22 2582 6630 2348851
Dysphagia 46.03 42.54 27 2577 12778 2342703
Hypokalaemia 45.11 42.54 25 2579 10629 2344852
Squamous cell carcinoma 45.00 42.54 14 2590 1369 2354112
Gamma-glutamyltransferase increased 44.16 42.54 20 2584 5542 2349939
Blood alkaline phosphatase increased 44.08 42.54 21 2583 6524 2348957
Oedema peripheral 43.73 42.54 33 2571 23730 2331751
Pneumonitis 43.45 42.54 18 2586 4021 2351460
Hepatocellular injury 43.38 42.54 18 2586 4037 2351444
Pain 43.21 42.54 50 2554 61807 2293674
Palmar-plantar erythrodysaesthesia syndrome 42.77 42.54 18 2586 4183 2351298

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 2130.19 38.35 689 2268 45711 1698113
Malignant neoplasm progression 833.50 38.35 259 2698 13899 1729925
Chills 670.32 38.35 210 2747 11477 1732347
Death 481.23 38.35 299 2658 87144 1656680
Metastatic malignant melanoma 405.21 38.35 75 2882 366 1743458
Metastases to central nervous system 374.35 38.35 87 2870 1458 1742366
Ejection fraction decreased 278.88 38.35 74 2883 2171 1741653
Fatigue 259.46 38.35 167 2790 50614 1693210
Rash 247.53 38.35 147 2810 38546 1705278
Malignant melanoma 204.16 38.35 54 2903 1559 1742265
Nausea 195.79 38.35 141 2816 51055 1692769
Basal cell carcinoma 168.14 38.35 51 2906 2432 1741392
Vomiting 149.41 38.35 107 2850 38208 1705616
Decreased appetite 139.81 38.35 86 2871 23785 1720039
Dehydration 127.85 38.35 73 2884 17585 1726239
Visual impairment 122.37 38.35 51 2906 6167 1737657
General physical health deterioration 121.94 38.35 64 2893 13054 1730770
Uveitis 117.85 38.35 32 2925 1019 1742805
Diarrhoea 115.32 38.35 106 2851 53746 1690078
C-reactive protein increased 111.54 38.35 47 2910 5838 1737986
Disease progression 108.12 38.35 65 2892 17198 1726626
Blood creatine phosphokinase increased 108.11 38.35 52 2905 8804 1735020
Metastases to liver 101.48 38.35 34 2923 2233 1741591
Squamous cell carcinoma 95.54 38.35 31 2926 1840 1741984
Headache 94.20 38.35 78 2879 34298 1709526
Malignant melanoma stage IV 93.90 38.35 15 2942 22 1743802
Asthenia 93.62 38.35 78 2879 34592 1709232
Product use in unapproved indication 90.41 38.35 47 2910 9375 1734449
Arthralgia 85.41 38.35 63 2894 23381 1720443
Hyperkeratosis 74.01 38.35 20 2937 624 1743200
Second primary malignancy 72.67 38.35 22 2935 1037 1742787
Vision blurred 69.46 38.35 38 2919 8385 1735439
Hypotension 68.33 38.35 61 2896 29593 1714231
Confusional state 68.19 38.35 53 2904 21225 1722599
Neutropenia 66.27 38.35 49 2908 18211 1725613
Metastases to bone 65.79 38.35 23 2934 1715 1742109
Panniculitis 64.80 38.35 14 2943 163 1743661
Metastases to skin 64.69 38.35 13 2944 103 1743721
Metastases to meninges 63.04 38.35 15 2942 276 1743548
Atrial fibrillation 62.71 38.35 44 2913 15067 1728757
Thrombocytopenia 61.80 38.35 50 2907 21199 1722625
Chorioretinopathy 58.30 38.35 15 2942 385 1743439
Pain 57.76 38.35 53 2904 26604 1717220
Hepatic enzyme increased 57.71 38.35 31 2926 6590 1737234
Cough 53.33 38.35 44 2913 19153 1724671
Leukopenia 53.14 38.35 32 2925 8448 1735376
Squamous cell carcinoma of skin 53.07 38.35 18 2939 1224 1742600
Abdominal pain 51.01 38.35 45 2912 21445 1722379
Acute kidney injury 50.88 38.35 56 2901 34888 1708936
Blood lactate dehydrogenase increased 49.11 38.35 23 2934 3652 1740172
Malaise 47.63 38.35 50 2907 29515 1714309
Metastases to lymph nodes 46.85 38.35 15 2942 851 1742973
Influenza like illness 46.28 38.35 26 2931 6027 1737797
Aspartate aminotransferase increased 46.18 38.35 32 2925 10724 1733100
Anaemia 45.99 38.35 49 2908 29408 1714416
Rash maculo-papular 45.88 38.35 22 2935 3681 1740143
Metastases to lung 45.65 38.35 17 2940 1518 1742306
Hepatocellular injury 45.59 38.35 21 2936 3210 1740614
Hyponatraemia 43.94 38.35 29 2928 8971 1734853
Rhabdomyolysis 42.99 38.35 31 2926 11059 1732765
Pneumonia 42.89 38.35 59 2898 46123 1697701
Electrocardiogram QT prolonged 42.89 38.35 24 2933 5521 1738303
Night sweats 42.46 38.35 18 2939 2258 1741566
Alanine aminotransferase increased 42.37 38.35 32 2925 12246 1731578
Liver function test increased 41.98 38.35 16 2941 1523 1742301
Pneumonitis 41.76 38.35 21 2936 3894 1739930
Epilepsy 41.53 38.35 21 2936 3938 1739886
Concomitant disease aggravated 40.55 38.35 13 2944 740 1743084
Brain oedema 39.75 38.35 17 2940 2179 1741645
Body temperature increased 39.66 38.35 18 2939 2659 1741165
Blood alkaline phosphatase increased 38.86 38.35 22 2935 5173 1738651
Papilloedema 38.39 38.35 12 2945 629 1743195

Pharmacologic Action:

SourceCodeDescription
ATC L01XE23 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
FDA MoA N0000185506 Cytochrome P450 3A4 Inducers
FDA MoA N0000187064 Cytochrome P450 2B6 Inducers
FDA MoA N0000187063 Cytochrome P450 2C8 Inducers
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers
FDA MoA N0000185607 Cytochrome P450 2C19 Inducers
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190110 Organic Anion Transporter 1 Inhibitors
FDA MoA N0000190111 Organic Anion Transporter 3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.56 acidic
pKa2 3.35 Basic
pKa3 0.43 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8835443 June 10, 2025 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 IMPROVEMENT OF GLYCEMIC CONTROL IN TYPE 2 DIABETES PATIENTS BY ADMINISTERING A STARTING DOSE OF 10 MCG FOR 14 DAYS AND INCREASING TO A MAINTENANCE DOSE OF 20 MCG ON DAY 15
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 IMPROVEMENT OF GLYCEMIC CONTROL IN TYPE 2 DIABETES PATIENTS BY ADMINISTERING A STARTING DOSE OF 10 MCG FOR 14 DAYS AND INCREASING TO A MAINTENANCE DOSE OF 20 MCG ON DAY 15
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 9233956 May 4, 2029 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 7994185 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8415345 Jan. 20, 2030 TREATMENT OF MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 IMPROVEMENT OF GLYCEMIC CONTROL IN TYPE 2 DIABETES PATIENTS BY ADMINISTERING A STARTING DOSE OF 10 MCG FOR 14 DAYS AND INCREASING TO A MAINTENANCE DOSE OF 20 MCG ON DAY 15
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8952018 Oct. 15, 2030 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 IMPROVEMENT OF GLYCEMIC CONTROL IN TYPE 2 DIABETES PATIENTS BY ADMINISTERING A STARTING DOSE OF 10 MCG FOR 14 DAYS AND INCREASING TO A MAINTENANCE DOSE OF 20 MCG ON DAY 15
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8703781 Oct. 15, 2030 TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 8952018 Oct. 15, 2030 TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST.

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL May 29, 2020 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA APPROVED TEST.
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL May 29, 2020 TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA APPROVED TEST.
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL 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 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE 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 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Jan. 9, 2021 DABRAFENIB IN COMBO WITH TRAMETINIB 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 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Jan. 9, 2021 DABRAFENIB IN COMBO WITH TRAMETINIB 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 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE 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 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE 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 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE 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 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE 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 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Oct. 6, 2022 ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL Oct. 6, 2022 ADDITION OF STUDY BRF117277, A NON-RANDOMIZED, OPEN-LABEL, MULTI-CENTER, MULTI-COHORT TRIAL OF DABRAFENIB PLUS TRAMETINIB IN SUBJECTS WITH BRAF MUTATION-POSITIVE MELANOMA THAT HAS METASTASIZED TO THE BRAIN
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL June 22, 2024 DABRAFENIB IN COMBINATION WITH TRAMETINIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL June 22, 2024 DABRAFENIB IN COMBINATION WITH TRAMETINIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL April 30, 2025 TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL April 30, 2025 TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 50MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL May 4, 2025 TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 75MG BASE TAFINLAR NOVARTIS N202806 May 29, 2013 RX CAPSULE ORAL May 4, 2025 TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Serine/threonine-protein kinase B-raf Kinase INHIBITOR IC50 9.15 WOMBAT-PK CHEMBL
TGF-beta receptor type-1 Kinase IC50 5.43 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase IC50 6.82 CHEMBL
Serine/threonine-protein kinase A-Raf Kinase IC50 7.59 CHEMBL

External reference:

IDSource
D10064 KEGG_DRUG
C3644554 UMLSCUI
B6DC89I63E UNII
1195768-06-9 SECONDARY_CAS_RN
9458 INN_ID
P06 PDB_CHEM_ID
DB08912 DRUGBANK_ID
CHEBI:75045 CHEBI
6494 IUPHAR_LIGAND_ID
C561627 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2028663 ChEMBL_ID
CHEMBL2105729 ChEMBL_ID
44462760 PUBCHEM_CID
703646006 SNOMEDCT_US
1424911 RXNORM
29476 MMSL
d08103 MMSL
015042 NDDF
4032496 VANDF
703641001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-0681 CAPSULE 75 mg ORAL NDA 18 sections
Tafinlar HUMAN PRESCRIPTION DRUG LABEL 1 0078-0682 CAPSULE 50 mg ORAL NDA 18 sections