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

Stem definitionDrug idCAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors 5289 1269440-17-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • encorafenib
  • braftovi
  • NVP-LGX818-NXA
Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF. Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Encorafenib was also able to bind to other kinases in vitro including JNK1, JNK2, JNK3, LIMK1, LIMK2, MEK4, and STK36 and substantially reduce ligand binding to these kinases at clinically achievable concentrations. Encorafenib inhibited in vitro growth of tumor cell lines expressing BRAF V600 E, D, and K mutations. In mice implanted with tumor cells expressing BRAF V600E, encorafenib induced tumor regressions associated with RAF/MEK/ERK pathway suppression.
  • Molecular weight: 540.01
  • Formula: C22H27ClFN7O4S
  • CLOGP: 2.88
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 140.13
  • ALOGS: -4.68
  • ROTB: 9
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.45 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 8, 2019 PMDA Ono Pharmaceutical Co., Ltd.
June 27, 2018 FDA ARRAY BIOPHARMA INC

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
Serous retinal detachment 923.34 26.86 132 6298 502 90621515
Neoplasm progression 342.89 26.86 126 6304 44360 90577657
Death 166.31 26.86 182 6248 456369 90165648
Off label use 161.20 26.86 282 6148 1101970 89520047
Retinal detachment 132.78 26.86 39 6391 6783 90615234
Serous retinopathy 112.18 26.86 15 6415 29 90621988
Second primary malignancy 104.86 26.86 36 6394 10342 90611675
Nausea 104.81 26.86 237 6193 1110079 89511938
Colitis 99.78 26.86 62 6368 69880 90552137
Pyrexia 93.22 26.86 167 6263 660318 89961699
Melanocytic naevus 76.68 26.86 24 6406 5162 90616855
Vision blurred 72.31 26.86 61 6369 110232 90511785
Decreased appetite 70.10 26.86 108 6322 376432 90245585
Malignant neoplasm progression 69.84 26.86 59 6371 106811 90515206
Uveitis 66.34 26.86 29 6401 15874 90606143
Dermatitis acneiform 64.02 26.86 22 6408 6332 90615685
Hepatic function abnormal 58.42 26.86 38 6392 46250 90575767
Diarrhoea 56.70 26.86 170 6260 939020 89682997
Tumour lysis syndrome 55.33 26.86 23 6407 11129 90610888
Retinopathy 54.95 26.86 17 6413 3517 90618500
Macular detachment 54.63 26.86 9 6421 99 90621918
Macular oedema 53.38 26.86 18 6412 4891 90617126
Blood creatine phosphokinase increased 53.19 26.86 32 6398 33991 90588026
Drug ineffective 45.29 26.86 21 6409 1384277 89237740
Large intestinal ulcer 45.12 26.86 15 6415 3902 90618115
Hospice care 41.46 26.86 18 6412 9686 90612331
Palmar-plantar erythrodysaesthesia syndrome 40.32 26.86 25 6405 27998 90594019
Vomiting 36.87 26.86 131 6299 788162 89833855
Detachment of retinal pigment epithelium 35.31 26.86 8 6422 497 90621520
Immune-mediated hepatitis 32.82 26.86 11 6419 2933 90619084
Colour blindness acquired 31.94 26.86 6 6424 146 90621871
Intestinal obstruction 31.70 26.86 24 6406 37107 90584910
Vogt-Koyanagi-Harada disease 31.35 26.86 7 6423 407 90621610
Visual impairment 30.39 26.86 42 6388 132323 90489694
Lipase increased 29.99 26.86 15 6415 11096 90610921
Myalgia 29.40 26.86 48 6382 175077 90446940
Ocular toxicity 29.29 26.86 8 6422 1069 90620948
Anaemia 29.28 26.86 72 6358 352730 90269287
Disease progression 29.14 26.86 45 6385 156570 90465447

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
Serous retinal detachment 791.62 24.18 135 6308 809 42614083
Neoplasm progression 375.31 24.18 147 6296 28853 42586039
Second primary malignancy 128.74 24.18 50 6393 9525 42605367
Serous retinopathy 125.86 24.18 23 6420 213 42614679
Death 104.56 24.18 223 6220 470962 42143930
Dermatitis acneiform 65.33 24.18 29 6414 7710 42607182
Off label use 63.29 24.18 225 6218 638110 41976782
Fatigue 60.85 24.18 173 6270 435468 42179424
Pyrexia 58.45 24.18 160 6283 393882 42221010
Nausea 57.75 24.18 160 6283 396639 42218253
Blood creatine phosphokinase increased 55.55 24.18 51 6392 48287 42566605
Melanocytic naevus 52.50 24.18 19 6424 2973 42611919
Malignant neoplasm progression 49.72 24.18 71 6372 108329 42506563
Vision blurred 47.34 24.18 49 6394 53650 42561242
Retinal detachment 47.33 24.18 22 6421 6503 42608389
Visual impairment 44.75 24.18 43 6400 43070 42571822
Uveitis 40.04 24.18 22 6421 9236 42605656
Subretinal fluid 39.55 24.18 11 6432 732 42614160
Macular oedema 38.79 24.18 16 6427 3553 42611339
Retinopathy 38.21 24.18 14 6429 2267 42612625
Diarrhoea 36.79 24.18 152 6291 460697 42154195
Decreased appetite 34.20 24.18 84 6359 193053 42421839
Metastases to central nervous system 32.54 24.18 20 6423 10335 42604557
Palmar-plantar erythrodysaesthesia syndrome 32.35 24.18 26 6417 20556 42594336
Ocular toxicity 31.51 24.18 8 6435 374 42614518
Polyneuropathy 30.24 24.18 24 6419 18637 42596255
Colitis 29.85 24.18 36 6407 46536 42568356
Retinal oedema 28.22 24.18 9 6434 959 42613933
Detachment of retinal pigment epithelium 27.80 24.18 8 6435 602 42614290
Liver disorder 27.65 24.18 32 6411 39612 42575280
Renal impairment 27.46 24.18 55 6388 110173 42504719

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Serous retinal detachment 1663.56 21.82 265 11985 1407 110575642
Neoplasm progression 665.90 21.82 255 11995 64340 110512709
Death 302.56 21.82 378 11872 698491 109878558
Second primary malignancy 213.62 21.82 79 12171 17989 110559060
Serous retinopathy 204.68 21.82 34 12216 241 110576808
Off label use 187.62 21.82 469 11781 1499716 109077333
Retinal detachment 155.39 21.82 55 12195 11045 110566004
Dermatitis acneiform 130.06 21.82 50 12200 12645 110564404
Nausea 130.04 21.82 363 11887 1235327 109341722
Pyrexia 123.40 21.82 292 11958 897973 109679076
Melanocytic naevus 118.69 21.82 38 12212 5616 110571433
Vision blurred 115.04 21.82 103 12147 128919 110448130
Blood creatine phosphokinase increased 109.28 21.82 79 12171 72998 110504051
Colitis 103.93 21.82 88 12162 102235 110474814
Malignant neoplasm progression 100.91 21.82 110 12140 174457 110402592
Decreased appetite 96.93 21.82 182 12068 475664 110101385
Uveitis 95.20 21.82 47 12203 21663 110555386
Retinopathy 93.93 21.82 30 12220 4399 110572650
Macular oedema 84.30 21.82 31 12219 6935 110570114
Diarrhoea 78.57 21.82 290 11960 1139215 109437834
Hepatic function abnormal 65.51 21.82 64 12186 89231 110487818
Visual impairment 62.92 21.82 76 12174 134352 110442697
Fatigue 61.97 21.82 282 11968 1215676 109361373
Macular detachment 60.61 21.82 12 12238 244 110576805
Large intestinal ulcer 60.11 21.82 23 12227 5738 110571311
Drug ineffective 59.52 21.82 49 12201 1520491 109056558
Subretinal fluid 59.00 21.82 16 12234 1328 110575721
Retinal oedema 55.97 21.82 16 12234 1611 110575438
Lipase increased 55.03 21.82 31 12219 18641 110558408
Detachment of retinal pigment epithelium 53.80 21.82 14 12236 991 110576058
Palmar-plantar erythrodysaesthesia syndrome 53.79 21.82 41 12209 40984 110536065
Renal impairment 51.22 21.82 82 12168 188363 110388686
Hospice care 48.80 21.82 25 12225 12448 110564601
Hepatic cytolysis 47.14 21.82 43 12207 55010 110522039
Tumour lysis syndrome 45.33 21.82 33 12217 30768 110546281
Metastases to central nervous system 44.32 21.82 29 12221 22788 110554261
Myalgia 41.38 21.82 82 12168 222299 110354750
Colour blindness acquired 41.38 21.82 8 12242 143 110576906
Vomiting 39.56 21.82 202 12048 910473 109666576
Disease progression 37.27 21.82 83 12167 243951 110333098
Aspartate aminotransferase increased 36.01 21.82 64 12186 159872 110417177
Cystoid macular oedema 35.88 21.82 13 12237 2787 110574262
Alanine aminotransferase increased 34.47 21.82 68 12182 183705 110393344
Amylase increased 32.13 21.82 19 12231 12500 110564549
Demyelinating polyneuropathy 30.92 21.82 11 12239 2238 110574811
Liver disorder 30.84 21.82 56 12194 142187 110434862
Immune-mediated hepatitis 30.82 21.82 15 12235 6696 110570353
Nasopharyngitis 30.19 21.82 4 12246 394357 110182692
Underdose 29.82 21.82 36 12214 63518 110513531
Hypothyroidism 28.97 21.82 38 12212 72861 110504188
Rash maculo-papular 28.43 21.82 38 12212 74184 110502865
Acute kidney injury 28.26 21.82 142 12108 635288 109941761
Lentigo 28.23 21.82 8 12242 780 110576269
Eye symptom 27.85 21.82 6 12244 187 110576862
Immune-mediated enterocolitis 27.57 21.82 16 12234 10169 110566880
Eye disorder 27.56 21.82 24 12226 28882 110548167
Metamorphopsia 26.35 21.82 9 12241 1624 110575425
Vogt-Koyanagi-Harada disease 25.49 21.82 7 12243 609 110576440
Enterocolitis 24.97 21.82 19 12231 18930 110558119
Neoplasm recurrence 24.95 21.82 12 12238 5220 110571829
Joint swelling 24.86 21.82 9 12241 442836 110134213
Malignant melanoma 24.63 21.82 18 12232 16873 110560176
Iridocyclitis 24.57 21.82 12 12238 5396 110571653
Gamma-glutamyltransferase increased 24.42 21.82 32 12218 61277 110515772
Drug hypersensitivity 24.21 21.82 10 12240 454080 110122969
Paronychia 23.78 21.82 15 12235 11066 110565983
Sinusitis 22.72 21.82 3 12247 296685 110280364
Depression 22.50 21.82 4 12246 317331 110259718
Blood creatinine increased 22.28 21.82 57 12193 182832 110394217
Toxicity to various agents 21.97 21.82 13 12237 480542 110096507

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EC03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
B-Raf serine-threonine kinase (BRAF) inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01EC B-Raf serine-threonine kinase (BRAF) inhibitors 3 drugs
dabrafenibtovorafenibvemurafenib

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

DiseaseRelationSNOMED_IDDOID
Metastatic malignant melanoma indication 443493003
Unresectable malignant melanoma with BRAF gene mutation indication 830150003
BRAF mutation-positive colorectal cancer indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.37 acidic
pKa2 13.42 acidic
pKa3 3.69 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 8541575 Feb. 26, 2030 TREATMENT OF MELANOMA
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON SMALL CELL LUNG CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA- APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 8541575 Feb. 26, 2030 TREATMENT OF MELANOMA
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 10005761 Aug. 27, 2030 TREATMENT OF MELANOMA
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 9850229 Aug. 27, 2030 INDICATED IN COMBINATION WITH BINIMETINIB FOR THE TREATMENT OF MELANOMA WITH A BRAF MUTATION
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 9850230 Aug. 27, 2030 TREATMENT OF MELANOMA WITH A BRAF MUTATION
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON SMALL CELL LUNG CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA- APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10005761 Aug. 27, 2030 TREATMENT OF MELANOMA
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850229 Aug. 27, 2030 INDICATED IN COMBINATION WITH BINIMETINIB FOR THE TREATMENT OF MELANOMA WITH A BRAF MUTATION
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON SMALL CELL LUNG CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA- APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9850230 Aug. 27, 2030 TREATMENT OF MELANOMA WITH A BRAF MUTATION
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 9314464 July 4, 2031 TREATMENT OF MELANOMA MEDIATED BY A B-RAF PROTEIN KINASE
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON SMALL CELL LUNG CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA- APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9314464 July 4, 2031 TREATMENT OF MELANOMA MEDIATED BY A B-RAF PROTEIN KINASE
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL 9763941 Nov. 21, 2032 TREATMENT OF MELANOMA
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10258622 Nov. 21, 2032 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST, AS CLAIMED
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10258622 Nov. 21, 2032 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 10258622 Nov. 21, 2032 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9763941 Nov. 21, 2032 TREATMENT OF MELANOMA
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9474754 Aug. 5, 2033 BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9474754 Aug. 5, 2033 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL 9474754 Aug. 5, 2033 BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL Oct. 11, 2026 ENCORAFENIB IN COMBINATION WITH BINIMETINIB, IS INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL Oct. 11, 2026 ENCORAFENIB IN COMBINATION WITH BINIMETINIB, IS INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL Dec. 20, 2027 IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL Dec. 20, 2027 IN COMBINATION WITH CETUXIMAB AND MFOLFOX6, FOR THE TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
50MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 DISCN CAPSULE ORAL Oct. 11, 2030 TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST
75MG BRAFTOVI ARRAY BIOPHARMA INC N210496 June 27, 2018 RX CAPSULE ORAL Oct. 11, 2030 TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
RAF proto-oncogene serine/threonine-protein kinase Kinase INHIBITOR IC50 9.52 DRUG LABEL DRUG LABEL
Serine/threonine-protein kinase B-raf Kinase INHIBITOR IC50 9.33 DRUG LABEL DRUG LABEL
Mitogen-activated protein kinase 14 Kinase IC50 5.66 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 5.84 CHEMBL
Glycogen synthase kinase-3 beta Kinase Kd 6.37 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.49 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 6.04 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 5.28 CHEMBL
MAP kinase-activated protein kinase 2 Kinase Kd 4.83 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 6.11 CHEMBL
LIM domain kinase 2 Kinase Kd 7.02 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.73 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 6.09 CHEMBL
Casein kinase I isoform alpha Kinase Kd 5.48 CHEMBL
Cyclin-dependent kinase 4 Kinase Kd 6.95 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.61 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.48 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 6.01 CHEMBL
Membrane-associated progesterone receptor component 1 Enzyme Kd 6.69 CHEMBL
Choline-phosphate cytidylyltransferase A Enzyme Kd 7.39 CHEMBL
Serine/threonine-protein kinase NLK Kinase Kd 6.13 CHEMBL
LIM domain kinase 1 Kinase Kd 7.58 CHEMBL

External reference:

IDSource
8L7891MRB6 UNII
4037644 VANDF
C4079208 UMLSCUI
CHEBI:755294 CHEBI
CHEMBL3301612 ChEMBL_ID
50922675 PUBCHEM_CID
DB11718 DRUGBANK_ID
D11053 KEGG_DRUG
9816 INN_ID
C000601108 MESH_SUPPLEMENTAL_RECORD_UI
7908 IUPHAR_LIGAND_ID
772091004 SNOMEDCT_US
772201002 SNOMEDCT_US
283907 MMSL
34462 MMSL
d08817 MMSL
017615 NDDF
2049106 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRAFTOVI HUMAN PRESCRIPTION DRUG LABEL 1 70255-025 CAPSULE 75 mg ORAL NDA 33 sections
BRAFTOVI HUMAN PRESCRIPTION DRUG LABEL 1 70255-050 CAPSULE 50 mg ORAL Export only 1 sections