dabrafenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors | 4801 | 1195765-45-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 26, 2013 | EMA | Novartis Europharm Limited | |
| May 29, 2013 | FDA | NOVARTIS PHARMS CORP | |
| March 28, 2016 | PMDA | Novartis Pharma K.K. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pyrexia | 1347.94 | 19.84 | 969 | 12663 | 417804 | 55860631 |
| Malignant neoplasm progression | 750.30 | 19.84 | 362 | 13270 | 73225 | 56205210 |
| Chills | 374.99 | 19.84 | 259 | 13373 | 102345 | 56176090 |
| Metastatic malignant melanoma | 368.98 | 19.84 | 83 | 13549 | 1407 | 56277028 |
| Uveitis | 243.16 | 19.84 | 94 | 13538 | 11001 | 56267434 |
| Death | 237.44 | 19.84 | 348 | 13284 | 341078 | 55937357 |
| Malignant melanoma | 235.57 | 19.84 | 91 | 13541 | 10628 | 56267807 |
| Metastases to central nervous system | 231.51 | 19.84 | 93 | 13539 | 12043 | 56266392 |
| Panniculitis | 126.44 | 19.84 | 57 | 13575 | 9785 | 56268650 |
| Visual impairment | 118.66 | 19.84 | 116 | 13516 | 74086 | 56204349 |
| Malignant melanoma stage IV | 114.18 | 19.84 | 19 | 13613 | 52 | 56278383 |
| Ejection fraction decreased | 104.06 | 19.84 | 63 | 13569 | 19778 | 56258657 |
| Drug ineffective | 79.72 | 19.84 | 64 | 13568 | 918925 | 55359510 |
| Erythema nodosum | 75.52 | 19.84 | 31 | 13601 | 4234 | 56274201 |
| Rash | 73.89 | 19.84 | 274 | 13358 | 492773 | 55785662 |
| Blood creatine phosphokinase increased | 73.46 | 19.84 | 58 | 13574 | 27894 | 56250541 |
| Dermatitis acneiform | 64.96 | 19.84 | 28 | 13604 | 4316 | 56274119 |
| Anaplastic thyroid cancer | 58.01 | 19.84 | 10 | 13622 | 36 | 56278399 |
| Serous retinal detachment | 55.36 | 19.84 | 13 | 13619 | 268 | 56278167 |
| Vision blurred | 54.99 | 19.84 | 83 | 13549 | 82860 | 56195575 |
| Product use in unapproved indication | 54.32 | 19.84 | 111 | 13521 | 140711 | 56137724 |
| Second primary malignancy | 50.78 | 19.84 | 28 | 13604 | 7374 | 56271061 |
| Chorioretinopathy | 49.83 | 19.84 | 15 | 13617 | 819 | 56277616 |
| Skin toxicity | 46.90 | 19.84 | 22 | 13610 | 4131 | 56274304 |
| Vogt-Koyanagi-Harada disease | 46.49 | 19.84 | 10 | 13622 | 136 | 56278299 |
| Drug hypersensitivity | 46.34 | 19.84 | 6 | 13626 | 275199 | 56003236 |
| Hyperpyrexia | 45.40 | 19.84 | 20 | 13612 | 3248 | 56275187 |
| Nausea | 44.97 | 19.84 | 327 | 13305 | 763851 | 55514584 |
| Iridocyclitis | 41.90 | 19.84 | 17 | 13615 | 2252 | 56276183 |
| Off label use | 41.77 | 19.84 | 44 | 13588 | 556136 | 55722299 |
| Metastasis | 41.02 | 19.84 | 21 | 13611 | 4763 | 56273672 |
| Vomiting | 40.80 | 19.84 | 232 | 13400 | 497996 | 55780439 |
| Rash maculo-papular | 40.30 | 19.84 | 42 | 13590 | 28865 | 56249570 |
| Non-small cell lung cancer | 40.15 | 19.84 | 19 | 13613 | 3639 | 56274796 |
| Blood lactate dehydrogenase increased | 40.06 | 19.84 | 36 | 13596 | 20639 | 56257796 |
| BRAF V600E mutation positive | 39.64 | 19.84 | 7 | 13625 | 30 | 56278405 |
| Erythema multiforme | 39.24 | 19.84 | 26 | 13606 | 9528 | 56268907 |
| Metastases to lung | 38.96 | 19.84 | 28 | 13604 | 11690 | 56266745 |
| Metastases to meninges | 38.49 | 19.84 | 16 | 13616 | 2254 | 56276181 |
| Melanoma recurrent | 38.35 | 19.84 | 8 | 13624 | 93 | 56278342 |
| Cutaneous sarcoidosis | 37.01 | 19.84 | 10 | 13622 | 369 | 56278066 |
| Ganglioglioma | 36.74 | 19.84 | 6 | 13626 | 14 | 56278421 |
| Condition aggravated | 36.54 | 19.84 | 19 | 13613 | 344879 | 55933556 |
| Hyperkeratosis | 36.05 | 19.84 | 20 | 13612 | 5327 | 56273108 |
| Palmar-plantar erythrodysaesthesia syndrome | 33.74 | 19.84 | 33 | 13599 | 21032 | 56257403 |
| Rhabdomyolysis | 33.27 | 19.84 | 45 | 13587 | 40613 | 56237822 |
| Dehydration | 33.20 | 19.84 | 99 | 13533 | 158726 | 56119709 |
| Sinusitis | 31.62 | 19.84 | 5 | 13627 | 197576 | 56080859 |
| Aspartate aminotransferase increased | 30.51 | 19.84 | 64 | 13568 | 82538 | 56195897 |
| Haemophagocytic lymphohistiocytosis | 29.84 | 19.84 | 22 | 13610 | 9550 | 56268885 |
| Abdominal discomfort | 29.76 | 19.84 | 15 | 13617 | 277259 | 56001176 |
| Systemic inflammatory response syndrome | 28.28 | 19.84 | 17 | 13615 | 5261 | 56273174 |
| Non-small cell lung cancer recurrent | 27.93 | 19.84 | 6 | 13626 | 81 | 56278354 |
| Retinal detachment | 27.80 | 19.84 | 17 | 13615 | 5424 | 56273011 |
| Pneumonitis | 27.46 | 19.84 | 36 | 13596 | 31528 | 56246907 |
| Vitreous floaters | 27.44 | 19.84 | 17 | 13615 | 5550 | 56272885 |
| Myalgia | 27.30 | 19.84 | 82 | 13550 | 131943 | 56146492 |
| Arthropathy | 26.14 | 19.84 | 8 | 13624 | 200267 | 56078168 |
| Squamous cell carcinoma | 26.02 | 19.84 | 19 | 13613 | 8129 | 56270306 |
| Panniculitis lobular | 26.00 | 19.84 | 5 | 13627 | 37 | 56278398 |
| Paronychia | 24.20 | 19.84 | 15 | 13617 | 4903 | 56273532 |
| Discomfort | 24.05 | 19.84 | 3 | 13629 | 141758 | 56136677 |
| Decreased appetite | 23.34 | 19.84 | 110 | 13522 | 219121 | 56059314 |
| Alanine aminotransferase increased | 23.08 | 19.84 | 62 | 13570 | 93600 | 56184835 |
| Leukoderma | 22.31 | 19.84 | 5 | 13627 | 83 | 56278352 |
| Acute polyneuropathy | 22.24 | 19.84 | 6 | 13626 | 220 | 56278215 |
| Keratoacanthoma | 22.22 | 19.84 | 7 | 13625 | 445 | 56277990 |
| Electrocardiogram QT prolonged | 22.17 | 19.84 | 44 | 13588 | 54544 | 56223891 |
| Treatment failure | 21.89 | 19.84 | 7 | 13625 | 170385 | 56108050 |
| Hypersensitivity | 21.88 | 19.84 | 18 | 13614 | 256390 | 56022045 |
| Fall | 21.85 | 19.84 | 33 | 13599 | 357477 | 55920958 |
| Dry skin | 21.62 | 19.84 | 40 | 13592 | 47069 | 56231366 |
| Joint swelling | 21.60 | 19.84 | 23 | 13609 | 289777 | 55988658 |
| Astrocytoma | 21.58 | 19.84 | 5 | 13627 | 97 | 56278338 |
| C-reactive protein increased | 21.35 | 19.84 | 54 | 13578 | 78630 | 56199805 |
| Infective glossitis | 20.75 | 19.84 | 4 | 13628 | 30 | 56278405 |
| Blood alkaline phosphatase increased | 20.35 | 19.84 | 35 | 13597 | 38910 | 56239525 |
| General physical health deterioration | 20.10 | 19.84 | 88 | 13544 | 169922 | 56108513 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pyrexia | 1305.87 | 19.08 | 1093 | 13800 | 302747 | 31379704 |
| Malignant neoplasm progression | 673.17 | 19.08 | 433 | 14460 | 78565 | 31603886 |
| Metastatic malignant melanoma | 485.03 | 19.08 | 128 | 14765 | 2167 | 31680284 |
| Chills | 391.84 | 19.08 | 304 | 14589 | 73846 | 31608605 |
| Metastases to central nervous system | 373.52 | 19.08 | 139 | 14754 | 7497 | 31674954 |
| Malignant melanoma | 272.93 | 19.08 | 111 | 14782 | 7596 | 31674855 |
| Death | 205.51 | 19.08 | 492 | 14401 | 360077 | 31322374 |
| Ejection fraction decreased | 184.25 | 19.08 | 110 | 14783 | 17324 | 31665127 |
| Uveitis | 134.01 | 19.08 | 65 | 14828 | 6751 | 31675700 |
| Metastases to liver | 93.81 | 19.08 | 64 | 14829 | 12663 | 31669788 |
| Malignant melanoma stage IV | 83.74 | 19.08 | 16 | 14877 | 51 | 31682400 |
| Visual impairment | 82.59 | 19.08 | 87 | 14806 | 31192 | 31651259 |
| Second primary malignancy | 75.88 | 19.08 | 45 | 14848 | 6987 | 31675464 |
| Metastases to stomach | 74.15 | 19.08 | 15 | 14878 | 69 | 31682382 |
| Basal cell carcinoma | 69.53 | 19.08 | 62 | 14831 | 18117 | 31664334 |
| Off label use | 67.45 | 19.08 | 40 | 14853 | 347234 | 31335217 |
| Metastases to lung | 61.22 | 19.08 | 42 | 14851 | 8380 | 31674071 |
| Squamous cell carcinoma | 60.87 | 19.08 | 46 | 14847 | 10665 | 31671786 |
| Rash | 59.87 | 19.08 | 219 | 14674 | 201267 | 31481184 |
| Blood creatine phosphokinase increased | 59.05 | 19.08 | 85 | 14808 | 41889 | 31640562 |
| Melanoma recurrent | 56.08 | 19.08 | 13 | 14880 | 124 | 31682327 |
| Anaplastic thyroid cancer | 52.79 | 19.08 | 9 | 14884 | 11 | 31682440 |
| Chorioretinopathy | 51.84 | 19.08 | 21 | 14872 | 1418 | 31681033 |
| Hyperpyrexia | 50.53 | 19.08 | 24 | 14869 | 2377 | 31680074 |
| Blood lactate dehydrogenase increased | 49.14 | 19.08 | 54 | 14839 | 20285 | 31662166 |
| Metastases to peritoneum | 48.95 | 19.08 | 21 | 14872 | 1639 | 31680812 |
| Product use in unapproved indication | 48.17 | 19.08 | 128 | 14765 | 99043 | 31583408 |
| C-reactive protein increased | 45.72 | 19.08 | 82 | 14811 | 48568 | 31633883 |
| Metastases to skin | 45.42 | 19.08 | 14 | 14879 | 420 | 31682031 |
| Panniculitis | 44.17 | 19.08 | 20 | 14873 | 1776 | 31680675 |
| Hyperkeratosis | 42.51 | 19.08 | 24 | 14869 | 3396 | 31679055 |
| Serous retinal detachment | 42.38 | 19.08 | 14 | 14879 | 527 | 31681924 |
| Drug interaction | 40.41 | 19.08 | 24 | 14869 | 208519 | 31473932 |
| Metastases to meninges | 40.18 | 19.08 | 17 | 14876 | 1282 | 31681169 |
| Haemophagocytic lymphohistiocytosis | 39.14 | 19.08 | 37 | 14856 | 11641 | 31670810 |
| Erythema nodosum | 38.85 | 19.08 | 16 | 14877 | 1127 | 31681324 |
| Malignant mesenteric neoplasm | 38.36 | 19.08 | 8 | 14885 | 44 | 31682407 |
| Fatigue | 36.24 | 19.08 | 275 | 14618 | 334931 | 31347520 |
| Metastases to bone | 35.65 | 19.08 | 34 | 14859 | 10814 | 31671637 |
| Metastases to lymph nodes | 35.13 | 19.08 | 23 | 14870 | 4245 | 31678206 |
| Jejunal ulcer perforation | 35.13 | 19.08 | 8 | 14885 | 70 | 31682381 |
| Vision blurred | 33.58 | 19.08 | 66 | 14827 | 41849 | 31640602 |
| Metastasis | 33.47 | 19.08 | 21 | 14872 | 3603 | 31678848 |
| Procalcitonin increased | 33.01 | 19.08 | 16 | 14877 | 1657 | 31680794 |
| Drug ineffective | 31.64 | 19.08 | 89 | 14804 | 395484 | 31286967 |
| Toxicity to various agents | 30.97 | 19.08 | 24 | 14869 | 181463 | 31500988 |
| Metastases to heart | 30.20 | 19.08 | 8 | 14885 | 137 | 31682314 |
| Tissue infiltration | 29.72 | 19.08 | 7 | 14886 | 72 | 31682379 |
| Gastrointestinal wall thickening | 29.46 | 19.08 | 14 | 14879 | 1388 | 31681063 |
| Brain neoplasm | 29.27 | 19.08 | 18 | 14875 | 2982 | 31679469 |
| Omental necrosis | 29.25 | 19.08 | 6 | 14887 | 30 | 31682421 |
| Intestinal metastasis | 29.08 | 19.08 | 8 | 14885 | 159 | 31682292 |
| Mesenteric neoplasm | 28.92 | 19.08 | 6 | 14887 | 32 | 31682419 |
| Eastern Cooperative Oncology Group performance status | 28.77 | 19.08 | 6 | 14887 | 33 | 31682418 |
| Decreased appetite | 28.70 | 19.08 | 145 | 14748 | 153072 | 31529379 |
| Ureteral disorder | 28.44 | 19.08 | 8 | 14885 | 173 | 31682278 |
| Disease progression | 25.64 | 19.08 | 97 | 14796 | 90367 | 31592084 |
| Nausea | 25.43 | 19.08 | 238 | 14655 | 307709 | 31374742 |
| Anxiety | 25.03 | 19.08 | 6 | 14887 | 91027 | 31591424 |
| Papilloedema | 24.25 | 19.08 | 15 | 14878 | 2511 | 31679940 |
| Retinal detachment | 23.12 | 19.08 | 19 | 14874 | 4967 | 31677484 |
| Vomiting | 22.59 | 19.08 | 181 | 14712 | 223792 | 31458659 |
| Overdose | 22.47 | 19.08 | 6 | 14887 | 84658 | 31597793 |
| Iridocyclitis | 22.43 | 19.08 | 12 | 14881 | 1528 | 31680923 |
| Malignant melanoma stage III | 21.94 | 19.08 | 4 | 14889 | 9 | 31682442 |
| General physical health deterioration | 21.67 | 19.08 | 108 | 14785 | 113327 | 31569124 |
| Metastases to adrenals | 21.59 | 19.08 | 10 | 14883 | 935 | 31681516 |
| Depression | 21.32 | 19.08 | 8 | 14885 | 90807 | 31591644 |
| BRAF gene mutation | 21.26 | 19.08 | 5 | 14888 | 51 | 31682400 |
| Bacterial diarrhoea | 21.00 | 19.08 | 5 | 14888 | 54 | 31682397 |
| Tumour invasion | 20.59 | 19.08 | 7 | 14886 | 288 | 31682163 |
| Lung adenocarcinoma stage IV | 20.21 | 19.08 | 6 | 14887 | 158 | 31682293 |
| Leukoderma | 20.08 | 19.08 | 5 | 14888 | 66 | 31682385 |
| Abdominal lymphadenopathy | 19.95 | 19.08 | 9 | 14884 | 792 | 31681659 |
| Liver function test increased | 19.72 | 19.08 | 27 | 14866 | 12687 | 31669764 |
| Febrile neutropenia | 19.66 | 19.08 | 17 | 14876 | 121832 | 31560619 |
| BRAF V600E mutation positive | 19.33 | 19.08 | 4 | 14889 | 21 | 31682430 |
| Body temperature fluctuation | 19.25 | 19.08 | 11 | 14882 | 1592 | 31680859 |
| Inflammatory bowel disease | 19.23 | 19.08 | 13 | 14880 | 2530 | 31679921 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pyrexia | 1990.47 | 17.66 | 1604 | 21583 | 605348 | 70299909 |
| Malignant neoplasm progression | 1096.47 | 17.66 | 608 | 22579 | 121131 | 70784126 |
| Metastatic malignant melanoma | 613.03 | 17.66 | 153 | 23034 | 3011 | 70902246 |
| Chills | 523.20 | 17.66 | 409 | 22778 | 144377 | 70760880 |
| Metastases to central nervous system | 430.82 | 17.66 | 168 | 23019 | 14866 | 70890391 |
| Malignant melanoma | 379.53 | 17.66 | 150 | 23037 | 13750 | 70891507 |
| Uveitis | 302.63 | 17.66 | 130 | 23057 | 14715 | 70890542 |
| Death | 299.69 | 17.66 | 569 | 22618 | 509492 | 70395765 |
| Ejection fraction decreased | 293.26 | 17.66 | 160 | 23027 | 30602 | 70874655 |
| Malignant melanoma stage IV | 199.13 | 17.66 | 37 | 23150 | 155 | 70905102 |
| Blood creatine phosphokinase increased | 126.01 | 17.66 | 126 | 23061 | 61137 | 70844120 |
| Panniculitis | 125.74 | 17.66 | 64 | 23123 | 10612 | 70894645 |
| Squamous cell carcinoma | 101.81 | 17.66 | 62 | 23125 | 14542 | 70890715 |
| Second primary malignancy | 100.31 | 17.66 | 59 | 23128 | 12992 | 70892265 |
| Erythema nodosum | 97.10 | 17.66 | 41 | 23146 | 4440 | 70900817 |
| Blood lactate dehydrogenase increased | 96.75 | 17.66 | 85 | 23102 | 35042 | 70870215 |
| Chorioretinopathy | 93.64 | 17.66 | 33 | 23154 | 2192 | 70903065 |
| Off label use | 92.91 | 17.66 | 65 | 23122 | 742995 | 70162262 |
| Basal cell carcinoma | 87.75 | 17.66 | 79 | 23108 | 33619 | 70871638 |
| Drug ineffective | 87.17 | 17.66 | 108 | 23079 | 939644 | 69965613 |
| Serous retinal detachment | 87.15 | 17.66 | 25 | 23162 | 847 | 70904410 |
| Hyperpyrexia | 86.80 | 17.66 | 40 | 23147 | 5334 | 70899923 |
| Anaplastic thyroid cancer | 82.31 | 17.66 | 15 | 23172 | 55 | 70905202 |
| Metastases to lung | 80.54 | 17.66 | 56 | 23131 | 16428 | 70888829 |
| Metastases to liver | 80.18 | 17.66 | 67 | 23120 | 25811 | 70879446 |
| Rheumatoid arthritis | 78.89 | 17.66 | 4 | 23183 | 291801 | 70613456 |
| Rash | 77.56 | 17.66 | 351 | 22836 | 510211 | 70395046 |
| Haemophagocytic lymphohistiocytosis | 74.01 | 17.66 | 57 | 23130 | 19555 | 70885702 |
| Dermatitis acneiform | 72.87 | 17.66 | 42 | 23145 | 8903 | 70896354 |
| Melanoma recurrent | 71.45 | 17.66 | 16 | 23171 | 192 | 70905065 |
| Hyperkeratosis | 67.88 | 17.66 | 37 | 23150 | 7047 | 70898210 |
| Metastasis | 67.22 | 17.66 | 35 | 23152 | 6079 | 70899178 |
| C-reactive protein increased | 66.45 | 17.66 | 125 | 23062 | 110392 | 70794865 |
| Metastases to stomach | 62.80 | 17.66 | 15 | 23172 | 243 | 70905014 |
| BRAF V600E mutation positive | 61.10 | 17.66 | 11 | 23176 | 37 | 70905220 |
| Iridocyclitis | 60.76 | 17.66 | 27 | 23160 | 3308 | 70901949 |
| Metastases to meninges | 59.10 | 17.66 | 26 | 23161 | 3110 | 70902147 |
| Ganglioglioma | 57.19 | 17.66 | 10 | 23177 | 27 | 70905230 |
| Condition aggravated | 56.57 | 17.66 | 35 | 23152 | 427600 | 70477657 |
| Drug hypersensitivity | 52.33 | 17.66 | 11 | 23176 | 262448 | 70642809 |
| Visual impairment | 52.30 | 17.66 | 94 | 23093 | 80156 | 70825101 |
| Drug interaction | 52.15 | 17.66 | 30 | 23157 | 381411 | 70523846 |
| Rash maculo-papular | 52.05 | 17.66 | 73 | 23114 | 50472 | 70854785 |
| Skin toxicity | 51.30 | 17.66 | 31 | 23156 | 7167 | 70898090 |
| Procalcitonin increased | 50.31 | 17.66 | 22 | 23165 | 2594 | 70902663 |
| Cutaneous sarcoidosis | 48.70 | 17.66 | 14 | 23173 | 478 | 70904779 |
| Metastases to lymph nodes | 46.57 | 17.66 | 32 | 23155 | 9206 | 70896051 |
| Metastases to bone | 45.93 | 17.66 | 46 | 23141 | 22330 | 70882927 |
| Metastases to peritoneum | 45.27 | 17.66 | 23 | 23164 | 3796 | 70901461 |
| Retinal detachment | 44.28 | 17.66 | 30 | 23157 | 8437 | 70896820 |
| Decreased appetite | 44.25 | 17.66 | 207 | 22980 | 304573 | 70600684 |
| Vogt-Koyanagi-Harada disease | 43.73 | 17.66 | 11 | 23176 | 223 | 70905034 |
| Metastases to skin | 43.01 | 17.66 | 17 | 23170 | 1554 | 70903703 |
| Product use in unapproved indication | 42.77 | 17.66 | 157 | 23030 | 207321 | 70697936 |
| Toxicity to various agents | 41.87 | 17.66 | 38 | 23149 | 382134 | 70523123 |
| Vision blurred | 41.26 | 17.66 | 94 | 23093 | 94890 | 70810367 |
| Aspartate aminotransferase increased | 40.79 | 17.66 | 112 | 23075 | 126866 | 70778391 |
| Malignant mesenteric neoplasm | 39.98 | 17.66 | 8 | 23179 | 53 | 70905204 |
| Vomiting | 39.25 | 17.66 | 329 | 22858 | 592782 | 70312475 |
| Dehydration | 39.19 | 17.66 | 162 | 23025 | 225980 | 70679277 |
| BRAF gene mutation | 39.11 | 17.66 | 8 | 23179 | 60 | 70905197 |
| Detachment of retinal pigment epithelium | 38.97 | 17.66 | 13 | 23174 | 731 | 70904526 |
| Squamous cell carcinoma of skin | 37.49 | 17.66 | 32 | 23155 | 12680 | 70892577 |
| Demyelinating polyneuropathy | 35.90 | 17.66 | 15 | 23172 | 1582 | 70903675 |
| Malignant melanoma stage III | 35.87 | 17.66 | 7 | 23180 | 40 | 70905217 |
| Blood alkaline phosphatase increased | 34.91 | 17.66 | 66 | 23121 | 58455 | 70846802 |
| Jejunal ulcer perforation | 34.72 | 17.66 | 8 | 23179 | 110 | 70905147 |
| Non-small cell lung cancer | 34.41 | 17.66 | 23 | 23164 | 6324 | 70898933 |
| Overdose | 34.05 | 17.66 | 7 | 23180 | 169738 | 70735519 |
| Anxiety | 33.56 | 17.66 | 15 | 23172 | 220315 | 70684942 |
| Palmar-plantar erythrodysaesthesia syndrome | 33.11 | 17.66 | 45 | 23142 | 30202 | 70875055 |
| Pneumonitis | 33.10 | 17.66 | 62 | 23125 | 54535 | 70850722 |
| Metastases to adrenals | 32.47 | 17.66 | 13 | 23174 | 1229 | 70904028 |
| Intestinal metastasis | 31.98 | 17.66 | 9 | 23178 | 284 | 70904973 |
| Keratoacanthoma | 31.93 | 17.66 | 12 | 23175 | 957 | 70904300 |
| Sinusitis | 31.89 | 17.66 | 8 | 23179 | 169187 | 70736070 |
| Hypophysitis | 31.56 | 17.66 | 18 | 23169 | 3740 | 70901517 |
| Anaplastic astrocytoma | 31.27 | 17.66 | 8 | 23179 | 174 | 70905083 |
| Hypersensitivity | 30.08 | 17.66 | 19 | 23168 | 229793 | 70675464 |
| Eastern Cooperative Oncology Group performance status | 29.57 | 17.66 | 6 | 23181 | 43 | 70905214 |
| Omental necrosis | 29.33 | 17.66 | 6 | 23181 | 45 | 70905212 |
| General physical health deterioration | 29.02 | 17.66 | 153 | 23034 | 235878 | 70669379 |
| Abdominal lymphadenopathy | 28.93 | 17.66 | 12 | 23175 | 1242 | 70904015 |
| Gamma-glutamyltransferase increased | 28.80 | 17.66 | 56 | 23131 | 50629 | 70854628 |
| Hepatocellular injury | 28.76 | 17.66 | 53 | 23134 | 46038 | 70859219 |
| Nausea | 28.60 | 17.66 | 413 | 22774 | 851675 | 70053582 |
| Intentional product use issue | 28.59 | 17.66 | 3 | 23184 | 120139 | 70785118 |
| Therapeutic product effect incomplete | 28.51 | 17.66 | 3 | 23184 | 119879 | 70785378 |
| Palmoplantar keratoderma | 28.19 | 17.66 | 9 | 23178 | 440 | 70904817 |
| Mesenteric neoplasm | 27.27 | 17.66 | 6 | 23181 | 66 | 70905191 |
| Gastrointestinal wall thickening | 27.27 | 17.66 | 14 | 23173 | 2362 | 70902895 |
| Disease progression | 26.93 | 17.66 | 112 | 23075 | 156560 | 70748697 |
| Concomitant disease aggravated | 26.90 | 17.66 | 26 | 23161 | 12088 | 70893169 |
| Joint swelling | 26.74 | 17.66 | 26 | 23161 | 253185 | 70652072 |
| Weight increased | 26.63 | 17.66 | 24 | 23163 | 242307 | 70662950 |
| Autoimmune colitis | 26.61 | 17.66 | 12 | 23175 | 1522 | 70903735 |
| Alanine aminotransferase increased | 26.59 | 17.66 | 107 | 23080 | 147373 | 70757884 |
| Papilloedema | 26.46 | 17.66 | 19 | 23168 | 5859 | 70899398 |
| Rhabdomyolysis | 26.42 | 17.66 | 80 | 23107 | 95680 | 70809577 |
| Musculoskeletal stiffness | 25.95 | 17.66 | 8 | 23179 | 147752 | 70757505 |
| Product dose omission issue | 25.78 | 17.66 | 20 | 23167 | 217448 | 70687809 |
| Tumour invasion | 25.68 | 17.66 | 8 | 23179 | 361 | 70904896 |
| Blood pressure increased | 25.48 | 17.66 | 15 | 23172 | 188502 | 70716755 |
| Paronychia | 25.47 | 17.66 | 20 | 23167 | 7054 | 70898203 |
| Lipase increased | 25.32 | 17.66 | 28 | 23159 | 15218 | 70890039 |
| Non-small cell lung cancer recurrent | 25.02 | 17.66 | 6 | 23181 | 99 | 70905158 |
| Dyspnoea | 24.83 | 17.66 | 149 | 23038 | 769911 | 70135346 |
| Fall | 24.24 | 17.66 | 70 | 23117 | 444026 | 70461231 |
| Metastases to heart | 23.65 | 17.66 | 7 | 23180 | 265 | 70904992 |
| Myalgia | 23.56 | 17.66 | 113 | 23074 | 167779 | 70737478 |
| Astrocytoma | 23.50 | 17.66 | 7 | 23180 | 271 | 70904986 |
| Arthropathy | 23.18 | 17.66 | 10 | 23177 | 150047 | 70755210 |
| Ureteral disorder | 22.97 | 17.66 | 8 | 23179 | 513 | 70904744 |
| Influenza like illness | 22.34 | 17.66 | 59 | 23128 | 65272 | 70839985 |
| Insomnia | 22.26 | 17.66 | 23 | 23164 | 217783 | 70687474 |
| Intentional overdose | 22.08 | 17.66 | 3 | 23184 | 98432 | 70806825 |
| Psoriasis | 22.08 | 17.66 | 3 | 23184 | 98430 | 70806827 |
| Body temperature fluctuation | 21.99 | 17.66 | 14 | 23173 | 3545 | 70901712 |
| Erythema multiforme | 21.81 | 17.66 | 27 | 23160 | 16537 | 70888720 |
| Fatigue | 21.76 | 17.66 | 384 | 22803 | 823935 | 70081322 |
| Abdominal discomfort | 21.57 | 17.66 | 23 | 23164 | 214635 | 70690622 |
| Erysipelas | 21.47 | 17.66 | 21 | 23166 | 9903 | 70895354 |
| Lung adenocarcinoma stage IV | 21.31 | 17.66 | 7 | 23180 | 375 | 70904882 |
| Vitiligo | 21.27 | 17.66 | 11 | 23176 | 1884 | 70903373 |
| Disseminated intravascular coagulation | 20.17 | 17.66 | 38 | 23149 | 33560 | 70871697 |
| Treatment failure | 20.15 | 17.66 | 11 | 23176 | 144131 | 70761126 |
| Left ventricular dysfunction | 20.08 | 17.66 | 27 | 23160 | 17930 | 70887327 |
| Nasopharyngitis | 19.98 | 17.66 | 26 | 23161 | 222180 | 70683077 |
| Asthenia | 19.54 | 17.66 | 232 | 22955 | 457434 | 70447823 |
| Amylase increased | 19.16 | 17.66 | 20 | 23167 | 10188 | 70895069 |
| Therapy cessation | 18.88 | 17.66 | 37 | 23150 | 33639 | 70871618 |
| Brain oedema | 18.64 | 17.66 | 30 | 23157 | 23388 | 70881869 |
| Metastatic neoplasm | 18.61 | 17.66 | 14 | 23173 | 4634 | 70900623 |
| Peripheral motor neuropathy | 18.56 | 17.66 | 12 | 23175 | 3120 | 70902137 |
| Visual acuity reduced | 18.54 | 17.66 | 33 | 23154 | 27897 | 70877360 |
| Sarcoidosis | 18.16 | 17.66 | 16 | 23171 | 6611 | 70898646 |
| Small intestine carcinoma | 18.06 | 17.66 | 8 | 23179 | 972 | 70904285 |
| Swelling | 18.06 | 17.66 | 21 | 23166 | 188518 | 70716739 |
| Vitreous floaters | 18.00 | 17.66 | 16 | 23171 | 6688 | 70898569 |
| Panniculitis lobular | 17.94 | 17.66 | 4 | 23183 | 47 | 70905210 |
| Leukoderma | 17.85 | 17.66 | 5 | 23182 | 155 | 70905102 |
| Cerebral haemorrhage | 17.76 | 17.66 | 48 | 23139 | 53816 | 70851441 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EC02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS B-Raf serine-threonine kinase (BRAF) inhibitors |
| FDA MoA | N0000175076 | Protein Kinase Inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D047428 | Protein Kinase Inhibitors |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000185507 | Cytochrome P450 2C9 Inducers |
| FDA MoA | N0000185607 | Cytochrome P450 2C19 Inducers |
| FDA MoA | N0000187063 | Cytochrome P450 2C8 Inducers |
| FDA MoA | N0000187064 | Cytochrome P450 2B6 Inducers |
| FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
| FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
| FDA MoA | N0000190110 | Organic Anion Transporter 1 Inhibitors |
| FDA MoA | N0000190111 | Organic Anion Transporter 3 Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:75047 | BRAF inhibitors |
| CHEBI has role | CHEBI:149553 | anticoronaviral drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Metastatic malignant melanoma | indication | 443493003 | |
| Malignant Melanoma with BRAF V600E Mutation | indication | 830150003 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.56 | acidic |
| pKa2 | 3.35 | Basic |
| pKa3 | 0.43 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 9233956 | May 4, 2029 | TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATIONS AFTER CONFIRMING THE PRESENCE OF BRAF V600E MUTATION |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TREATMENT OF MELANOMA |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TREATMENT OF MELANOMA |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 7994185 | Jan. 20, 2030 | TREATMENT OF MELANOMA |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8415345 | Jan. 20, 2030 | TREATMENT OF MELANOMA |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8952018 | Oct. 15, 2030 | TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IN COMBINATION WITH TRAMETINIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8703781 | Oct. 15, 2030 | TAFINLAR IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 8952018 | Oct. 15, 2030 | TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST. |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 10869869 | Aug. 30, 2033 | TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | 10869869 | Aug. 30, 2033 | TAFINLAR(R) IS INDICATED, IN COMBINATION WITH TRAMETINIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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 |
| EQ 50MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | June 22, 2025 | DABRAFENIB IS INDICATED IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS |
| EQ 75MG BASE | TAFINLAR | NOVARTIS | N202806 | May 29, 2013 | RX | CAPSULE | ORAL | June 22, 2025 | DABRAFENIB IS INDICATED IN COMBINATION WITH TRAMETINIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase B-raf | Kinase | INHIBITOR | IC50 | 9.16 | WOMBAT-PK | CHEMBL | |||
| Tyrosine-protein kinase Lck | Kinase | Kd | 6.11 | CHEMBL | |||||
| Tyrosine-protein kinase Yes | Kinase | Kd | 5.89 | CHEMBL | |||||
| Tyrosine-protein kinase Fyn | Kinase | Kd | 6.09 | CHEMBL | |||||
| RAF proto-oncogene serine/threonine-protein kinase | Kinase | IC50 | 6.82 | CHEMBL | |||||
| Cyclin-dependent kinase 1 | Kinase | Kd | 6.44 | CHEMBL | |||||
| Cyclin-dependent kinase 2 | Kinase | Kd | 7.72 | CHEMBL | |||||
| Tyrosine-protein kinase HCK | Kinase | Kd | 5.78 | CHEMBL | |||||
| Tyrosine-protein kinase JAK2 | Kinase | Kd | 5.49 | CHEMBL | |||||
| Tyrosine-protein kinase CSK | Kinase | Kd | 6.07 | CHEMBL | |||||
| Hepatocyte growth factor receptor | Kinase | Kd | 5.79 | CHEMBL | |||||
| Tyrosine-protein kinase Lyn | Kinase | Kd | 5.87 | CHEMBL | |||||
| LIM domain kinase 1 | Kinase | Kd | 7.48 | CHEMBL | |||||
| Cyclin-dependent-like kinase 5 | Kinase | Kd | 5.97 | CHEMBL | |||||
| Serine/threonine-protein kinase PLK4 | Kinase | Kd | 6.28 | CHEMBL | |||||
| Abelson tyrosine-protein kinase 2 | Kinase | Kd | 6.52 | CHEMBL | |||||
| Tyrosine-protein kinase Fgr | Kinase | Kd | 5.81 | CHEMBL | |||||
| Tyrosine-protein kinase FRK | Kinase | Kd | 6.14 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 2 | Kinase | IC50 | 7.11 | CHEMBL | |||||
| Cyclin-dependent kinase 16 | Kinase | Kd | 7.89 | CHEMBL | |||||
| Activin receptor type-1B | Kinase | Kd | 6.22 | CHEMBL | |||||
| TGF-beta receptor type-2 | Kinase | Kd | 5.60 | CHEMBL | |||||
| Cyclin-dependent kinase 6 | Kinase | Kd | 6.50 | CHEMBL | |||||
| Protein-tyrosine kinase 6 | Kinase | Kd | 5.85 | CHEMBL | |||||
| Non-receptor tyrosine-protein kinase TNK1 | Kinase | Kd | 7.18 | CHEMBL | |||||
| Cyclin-dependent kinase 17 | Kinase | Kd | 7.44 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase MLT | Kinase | Kd | 6.74 | CHEMBL | |||||
| LIM domain kinase 2 | Kinase | Kd | 7.09 | CHEMBL | |||||
| Maternal embryonic leucine zipper kinase | Kinase | Kd | 5.74 | CHEMBL | |||||
| Serine/threonine-protein kinase SIK2 | Kinase | Kd | 6.19 | CHEMBL | |||||
| Calcium/calmodulin-dependent protein kinase type IV | Kinase | Kd | 5.64 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase 11 | Kinase | Kd | 6 | CHEMBL | |||||
| Serine/threonine-protein kinase Nek9 | Kinase | Kd | 7.28 | CHEMBL | |||||
| TGF-beta receptor type-1 | Kinase | IC50 | 5.43 | CHEMBL | |||||
| Ephrin type-A receptor 1 | Kinase | Kd | 6.15 | CHEMBL | |||||
| Serine/threonine-protein kinase D2 | Kinase | Kd | 7.47 | CHEMBL | |||||
| Serine/threonine-protein kinase D3 | Kinase | Kd | 6.92 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 1 | Kinase | IC50 | 4.27 | CHEMBL | |||||
| Cyclin-dependent kinase 4 | Kinase | Kd | 6.90 | CHEMBL | |||||
| Ephrin type-B receptor 6 | Kinase | Kd | 6.38 | CHEMBL | |||||
| Serine/threonine-protein kinase/endoribonuclease IRE1 | Kinase | Kd | 5.84 | CHEMBL | |||||
| Interleukin-1 receptor-associated kinase 1 | Kinase | Kd | 5.81 | CHEMBL | |||||
| Serine/threonine-protein kinase ULK1 | Kinase | Kd | 6.73 | CHEMBL | |||||
| Serine/threonine-protein kinase ULK3 | Kinase | Kd | 5.83 | CHEMBL | |||||
| Serine/threonine-protein kinase SIK3 | Kinase | Kd | 5.70 | CHEMBL | |||||
| Eukaryotic translation initiation factor 2-alpha kinase 1 | Kinase | Kd | 6.02 | CHEMBL | |||||
| Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 5.64 | CHEMBL | |||||
| Dual serine/threonine and tyrosine protein kinase | Kinase | IC50 | 4.53 | CHEMBL | |||||
| Serine/threonine-protein kinase A-Raf | Kinase | IC50 | 7.59 | CHEMBL | |||||
| GTPase KRas | Enzyme | IC50 | 5.23 | CHEMBL | |||||
| Serine/threonine-protein kinase Nek1 | Kinase | Kd | 6.32 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 3 | Kinase | IC50 | 8.70 | CHEMBL | |||||
| Tyrosine-protein kinase ABL1 | Kinase | Kd | 5.81 | CHEMBL | |||||
| Serine/threonine-protein kinase/endoribonuclease IRE2 | Kinase | Kd | 6.94 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10064 | KEGG_DRUG |
| 1195768-06-9 | SECONDARY_CAS_RN |
| 4032496 | VANDF |
| CHEBI:75045 | CHEBI |
| P06 | PDB_CHEM_ID |
| CHEMBL2028663 | ChEMBL_ID |
| CHEMBL2105729 | ChEMBL_ID |
| C561627 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6494 | IUPHAR_LIGAND_ID |
| 9458 | INN_ID |
| DB08912 | DRUGBANK_ID |
| QGP4HA4G1B | UNII |
| 1424911 | RXNORM |
| 203107 | MMSL |
| 29476 | MMSL |
| 29650 | MMSL |
| d08103 | MMSL |
| 015042 | NDDF |
| 015043 | NDDF |
| 703641001 | SNOMEDCT_US |
| 703642008 | SNOMEDCT_US |
| 703646006 | SNOMEDCT_US |
| C3467876 | UMLSCUI |
| CHEMBL523411 | ChEMBL_ID |
| 44462760 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0681 | CAPSULE | 75 mg | ORAL | NDA | 32 sections |
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0681 | CAPSULE | 75 mg | ORAL | NDA | 32 sections |
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0681 | CAPSULE | 75 mg | ORAL | NDA | 32 sections |
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0682 | CAPSULE | 50 mg | ORAL | NDA | 32 sections |
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0682 | CAPSULE | 50 mg | ORAL | NDA | 32 sections |
| Tafinlar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0682 | CAPSULE | 50 mg | ORAL | NDA | 32 sections |