| Stem definition | Drug id | CAS RN |
|---|---|---|
| Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors | 4185 | 918504-65-1 |
| Dose | Unit | Route |
|---|---|---|
| 1.92 | g | O |
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 17, 2011 | FDA | HOFFMANN LA ROCHE |
| 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 |
|---|---|---|---|---|---|---|
| Rash | 314.19 | 25.57 | 386 | 8459 | 560485 | 62919692 |
| Disease progression | 313.32 | 25.57 | 201 | 8644 | 122557 | 63357620 |
| Photosensitivity reaction | 239.95 | 25.57 | 87 | 8758 | 14907 | 63465270 |
| Metastases to central nervous system | 239.83 | 25.57 | 84 | 8761 | 13021 | 63467156 |
| Keratoacanthoma | 209.28 | 25.57 | 39 | 8806 | 444 | 63479733 |
| Rash maculo-papular | 179.60 | 25.57 | 88 | 8757 | 31808 | 63448369 |
| Sunburn | 174.13 | 25.57 | 46 | 8799 | 2742 | 63477435 |
| Drug reaction with eosinophilia and systemic symptoms | 168.82 | 25.57 | 86 | 8759 | 33750 | 63446427 |
| Skin toxicity | 167.42 | 25.57 | 50 | 8795 | 4664 | 63475513 |
| Squamous cell carcinoma | 145.22 | 25.57 | 52 | 8793 | 8580 | 63471597 |
| Hyperkeratosis | 131.20 | 25.57 | 44 | 8801 | 5974 | 63474203 |
| Skin papilloma | 127.12 | 25.57 | 41 | 8804 | 4928 | 63475249 |
| Erythema multiforme | 108.70 | 25.57 | 44 | 8801 | 10125 | 63470052 |
| Pyrexia | 108.43 | 25.57 | 216 | 8629 | 470262 | 63009915 |
| Arthralgia | 97.56 | 25.57 | 232 | 8613 | 569478 | 62910699 |
| Melanocytic naevus | 94.47 | 25.57 | 32 | 8813 | 4476 | 63475701 |
| Blood lactate dehydrogenase increased | 90.47 | 25.57 | 50 | 8795 | 23066 | 63457111 |
| Death | 86.21 | 25.57 | 172 | 8673 | 374209 | 63105968 |
| Electrocardiogram QT prolonged | 85.69 | 25.57 | 69 | 8776 | 59461 | 63420716 |
| Chorioretinopathy | 82.99 | 25.57 | 20 | 8825 | 819 | 63479358 |
| Squamous cell carcinoma of skin | 81.24 | 25.57 | 31 | 8814 | 6101 | 63474076 |
| Uveitis | 80.81 | 25.57 | 38 | 8807 | 12515 | 63467662 |
| Toxic skin eruption | 70.82 | 25.57 | 35 | 8810 | 12850 | 63467327 |
| Mass | 68.07 | 25.57 | 35 | 8810 | 13965 | 63466212 |
| Erythema | 65.52 | 25.57 | 100 | 8745 | 175651 | 63304526 |
| Metastatic malignant melanoma | 64.78 | 25.57 | 18 | 8827 | 1297 | 63478880 |
| Neutrophilic panniculitis | 54.47 | 25.57 | 9 | 8836 | 47 | 63480130 |
| Keratosis pilaris | 54.15 | 25.57 | 9 | 8836 | 49 | 63480128 |
| Stevens-Johnson syndrome | 54.05 | 25.57 | 37 | 8808 | 24913 | 63455264 |
| Solar dermatitis | 51.73 | 25.57 | 10 | 8835 | 140 | 63480037 |
| Serous retinal detachment | 48.14 | 25.57 | 11 | 8834 | 356 | 63479821 |
| Drug ineffective | 45.98 | 25.57 | 47 | 8798 | 1044718 | 62435459 |
| Panniculitis | 45.56 | 25.57 | 25 | 8820 | 11360 | 63468817 |
| Diarrhoea | 44.63 | 25.57 | 207 | 8638 | 715159 | 62765018 |
| Malignant neoplasm progression | 42.91 | 25.57 | 55 | 8790 | 82066 | 63398111 |
| Drug eruption | 42.83 | 25.57 | 34 | 8811 | 28660 | 63451517 |
| Decreased appetite | 42.40 | 25.57 | 102 | 8743 | 250950 | 63229227 |
| Papilloma | 40.58 | 25.57 | 9 | 8836 | 254 | 63479923 |
| Condition aggravated | 39.10 | 25.57 | 5 | 8840 | 402212 | 63077965 |
| Retinal detachment | 38.20 | 25.57 | 18 | 8827 | 5951 | 63474226 |
| Face oedema | 36.88 | 25.57 | 27 | 8818 | 20185 | 63459992 |
| Acrochordon | 36.45 | 25.57 | 11 | 8834 | 1061 | 63479116 |
| Erythema nodosum | 35.24 | 25.57 | 16 | 8829 | 4859 | 63475318 |
| Dermatitis acneiform | 34.87 | 25.57 | 16 | 8829 | 4980 | 63475197 |
| Decreased activity | 34.22 | 25.57 | 17 | 8828 | 6303 | 63473874 |
| Dermatitis exfoliative | 33.52 | 25.57 | 16 | 8829 | 5443 | 63474734 |
| Radiation skin injury | 33.46 | 25.57 | 10 | 8835 | 933 | 63479244 |
| Dysphagia | 32.38 | 25.57 | 50 | 8795 | 88535 | 63391642 |
| Enanthema | 31.29 | 25.57 | 8 | 8837 | 418 | 63479759 |
| Myalgia | 29.65 | 25.57 | 64 | 8781 | 146465 | 63333712 |
| Malignant melanoma in situ | 29.28 | 25.57 | 9 | 8836 | 923 | 63479254 |
| Dermatitis exfoliative generalised | 29.13 | 25.57 | 13 | 8832 | 3794 | 63476383 |
| Fall | 27.79 | 25.57 | 10 | 8835 | 392324 | 63087853 |
| Hepatocellular injury | 27.74 | 25.57 | 26 | 8819 | 27355 | 63452822 |
| Impaired work ability | 26.70 | 25.57 | 21 | 8824 | 17454 | 63462723 |
| 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 |
|---|---|---|---|---|---|---|
| Rash | 456.17 | 24.43 | 439 | 10180 | 222313 | 34723999 |
| Disease progression | 447.69 | 24.43 | 321 | 10298 | 107756 | 34838556 |
| Photosensitivity reaction | 392.30 | 24.43 | 140 | 10479 | 10454 | 34935858 |
| Sunburn | 338.71 | 24.43 | 84 | 10535 | 1739 | 34944573 |
| Metastases to central nervous system | 268.44 | 24.43 | 99 | 10520 | 8106 | 34938206 |
| Hyperkeratosis | 195.17 | 24.43 | 64 | 10555 | 3685 | 34942627 |
| Skin papilloma | 190.83 | 24.43 | 55 | 10564 | 2048 | 34944264 |
| Keratoacanthoma | 162.14 | 24.43 | 38 | 10581 | 612 | 34945700 |
| Squamous cell carcinoma | 158.89 | 24.43 | 75 | 10544 | 11400 | 34934912 |
| Alopecia | 152.70 | 24.43 | 94 | 10525 | 24261 | 34922051 |
| Skin toxicity | 142.80 | 24.43 | 54 | 10565 | 4730 | 34941582 |
| Arthralgia | 138.80 | 24.43 | 211 | 10408 | 169830 | 34776482 |
| Uveitis | 97.42 | 24.43 | 47 | 10572 | 7488 | 34938824 |
| Keratosis pilaris | 92.97 | 24.43 | 17 | 10602 | 70 | 34946242 |
| Pyrexia | 90.69 | 24.43 | 263 | 10356 | 332750 | 34613562 |
| Rash maculo-papular | 87.35 | 24.43 | 71 | 10548 | 28380 | 34917932 |
| Melanocytic naevus | 86.74 | 24.43 | 31 | 10588 | 2313 | 34943999 |
| Squamous cell carcinoma of skin | 68.15 | 24.43 | 42 | 10577 | 10839 | 34935473 |
| Dermatitis acneiform | 66.36 | 24.43 | 34 | 10585 | 6155 | 34940157 |
| Chorioretinopathy | 63.87 | 24.43 | 22 | 10597 | 1471 | 34944841 |
| Mass | 61.23 | 24.43 | 35 | 10584 | 7870 | 34938442 |
| Malignant melanoma | 57.83 | 24.43 | 34 | 10585 | 8056 | 34938256 |
| Blood lactate dehydrogenase increased | 53.53 | 24.43 | 49 | 10570 | 22941 | 34923371 |
| Iridocyclitis | 50.56 | 24.43 | 19 | 10600 | 1633 | 34944679 |
| Retinopathy | 49.90 | 24.43 | 20 | 10599 | 2044 | 34944268 |
| Drug reaction with eosinophilia and systemic symptoms | 48.73 | 24.43 | 55 | 10564 | 32957 | 34913355 |
| Intentional product use issue | 48.23 | 24.43 | 74 | 10545 | 59742 | 34886570 |
| Death | 46.82 | 24.43 | 241 | 10378 | 397808 | 34548504 |
| Serous retinal detachment | 46.70 | 24.43 | 14 | 10605 | 598 | 34945714 |
| Decreased appetite | 46.54 | 24.43 | 133 | 10486 | 166259 | 34780053 |
| Retinal detachment | 44.80 | 24.43 | 25 | 10594 | 5366 | 34940946 |
| Poor quality sleep | 44.53 | 24.43 | 29 | 10590 | 8227 | 34938085 |
| Neoplasm | 44.48 | 24.43 | 25 | 10594 | 5442 | 34940870 |
| Fatigue | 43.27 | 24.43 | 224 | 10395 | 370429 | 34575883 |
| Erythema | 42.04 | 24.43 | 87 | 10532 | 88693 | 34857619 |
| Dysphagia | 41.86 | 24.43 | 71 | 10548 | 62310 | 34884002 |
| Metastatic malignant melanoma | 39.81 | 24.43 | 17 | 10602 | 2038 | 34944274 |
| Rash follicular | 39.29 | 24.43 | 7 | 10612 | 24 | 34946288 |
| Impaired work ability | 38.99 | 24.43 | 25 | 10594 | 6905 | 34939407 |
| Dysgeusia | 38.85 | 24.43 | 44 | 10575 | 26453 | 34919859 |
| Solar dermatitis | 38.81 | 24.43 | 8 | 10611 | 68 | 34946244 |
| Skin reaction | 37.43 | 24.43 | 22 | 10597 | 5208 | 34941104 |
| Diarrhoea | 35.16 | 24.43 | 220 | 10399 | 389692 | 34556620 |
| No adverse event | 33.49 | 24.43 | 38 | 10581 | 22889 | 34923423 |
| Decreased activity | 32.84 | 24.43 | 19 | 10600 | 4368 | 34941944 |
| Acne | 32.64 | 24.43 | 27 | 10592 | 11039 | 34935273 |
| Hepatotoxicity | 32.04 | 24.43 | 36 | 10583 | 21449 | 34924863 |
| Panniculitis | 30.58 | 24.43 | 14 | 10605 | 1980 | 34944332 |
| Myalgia | 30.35 | 24.43 | 74 | 10545 | 84036 | 34862276 |
| Hyperthyroidism | 29.55 | 24.43 | 25 | 10594 | 10541 | 34935771 |
| Pruritus | 28.23 | 24.43 | 101 | 10518 | 141880 | 34804432 |
| Skin hypopigmentation | 27.74 | 24.43 | 8 | 10611 | 298 | 34946014 |
| Condition aggravated | 27.50 | 24.43 | 12 | 10607 | 192184 | 34754128 |
| Skin mass | 26.53 | 24.43 | 16 | 10603 | 3969 | 34942343 |
| Toxic skin eruption | 25.97 | 24.43 | 24 | 10595 | 11361 | 34934951 |
| Blood creatine phosphokinase increased | 24.87 | 24.43 | 47 | 10572 | 44810 | 34901502 |
| Serous retinopathy | 24.81 | 24.43 | 6 | 10613 | 111 | 34946201 |
| 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 |
|---|---|---|---|---|---|---|
| Photosensitivity reaction | 502.34 | 21.08 | 178 | 14943 | 20949 | 79708318 |
| Rash | 496.37 | 21.08 | 576 | 14545 | 577782 | 79151485 |
| Disease progression | 333.26 | 21.08 | 277 | 14844 | 184085 | 79545182 |
| Keratoacanthoma | 317.70 | 21.08 | 66 | 15055 | 979 | 79728288 |
| Sunburn | 278.30 | 21.08 | 76 | 15045 | 3757 | 79725510 |
| Rash maculo-papular | 277.03 | 21.08 | 157 | 14964 | 55921 | 79673346 |
| Hyperkeratosis | 265.24 | 21.08 | 86 | 15035 | 7704 | 79721563 |
| Skin toxicity | 255.74 | 21.08 | 85 | 15036 | 8229 | 79721038 |
| Squamous cell carcinoma | 220.46 | 21.08 | 90 | 15031 | 15532 | 79713735 |
| Pyrexia | 187.08 | 21.08 | 402 | 14719 | 678307 | 79050960 |
| Drug reaction with eosinophilia and systemic symptoms | 180.99 | 21.08 | 126 | 14995 | 64118 | 79665149 |
| Skin papilloma | 160.58 | 21.08 | 55 | 15066 | 5831 | 79723436 |
| Uveitis | 149.50 | 21.08 | 70 | 15051 | 16760 | 79712507 |
| Keratosis pilaris | 144.14 | 21.08 | 22 | 15099 | 39 | 79729228 |
| Melanocytic naevus | 135.98 | 21.08 | 46 | 15075 | 4695 | 79724572 |
| Metastases to central nervous system | 135.92 | 21.08 | 65 | 15056 | 16310 | 79712957 |
| Chorioretinopathy | 133.39 | 21.08 | 38 | 15083 | 2193 | 79727074 |
| Arthralgia | 128.65 | 21.08 | 313 | 14808 | 571490 | 79157777 |
| Squamous cell carcinoma of skin | 123.51 | 21.08 | 58 | 15063 | 13975 | 79715292 |
| Serous retinal detachment | 96.42 | 21.08 | 25 | 15096 | 1009 | 79728258 |
| Retinal detachment | 96.39 | 21.08 | 43 | 15078 | 9204 | 79720063 |
| Dermatitis acneiform | 87.00 | 21.08 | 41 | 15080 | 9952 | 79719315 |
| Toxic skin eruption | 77.82 | 21.08 | 50 | 15071 | 22243 | 79707024 |
| Erythema multiforme | 75.34 | 21.08 | 45 | 15076 | 17606 | 79711661 |
| Neutrophilic panniculitis | 73.29 | 21.08 | 13 | 15108 | 77 | 79729190 |
| Death | 71.86 | 21.08 | 253 | 14868 | 566261 | 79163006 |
| Solar dermatitis | 71.71 | 21.08 | 15 | 15106 | 230 | 79729037 |
| Erythema | 71.29 | 21.08 | 141 | 14980 | 223149 | 79506118 |
| Panniculitis | 67.44 | 21.08 | 37 | 15084 | 12334 | 79716933 |
| Diarrhoea | 66.91 | 21.08 | 336 | 14785 | 880153 | 78849114 |
| Retinopathy | 60.33 | 21.08 | 24 | 15097 | 3867 | 79725400 |
| Papilloma | 60.07 | 21.08 | 14 | 15107 | 360 | 79728907 |
| Iridocyclitis | 57.96 | 21.08 | 23 | 15098 | 3681 | 79725586 |
| Blood creatine phosphokinase increased | 57.95 | 21.08 | 67 | 15054 | 66023 | 79663244 |
| Condition aggravated | 56.39 | 21.08 | 13 | 15108 | 501111 | 79228156 |
| Malignant neoplasm progression | 56.14 | 21.08 | 96 | 15025 | 135894 | 79593373 |
| Electrocardiogram QT prolonged | 55.95 | 21.08 | 77 | 15044 | 90309 | 79638958 |
| Radiation skin injury | 53.58 | 21.08 | 17 | 15104 | 1417 | 79727850 |
| Stevens-Johnson syndrome | 52.83 | 21.08 | 50 | 15071 | 39116 | 79690151 |
| Drug ineffective | 50.22 | 21.08 | 80 | 15041 | 1080833 | 78648434 |
| Erythema nodosum | 49.95 | 21.08 | 23 | 15098 | 5294 | 79723973 |
| Decreased appetite | 48.63 | 21.08 | 159 | 14962 | 342259 | 79387008 |
| Malignant melanoma | 46.41 | 21.08 | 31 | 15090 | 14710 | 79714557 |
| Hyperthyroidism | 43.36 | 21.08 | 35 | 15086 | 22174 | 79707093 |
| Cholestasis | 42.64 | 21.08 | 51 | 15070 | 52058 | 79677209 |
| Metastatic malignant melanoma | 42.10 | 21.08 | 17 | 15104 | 2846 | 79726421 |
| Face oedema | 41.98 | 21.08 | 38 | 15083 | 28098 | 79701169 |
| Seborrhoeic keratosis | 41.68 | 21.08 | 16 | 15105 | 2344 | 79726923 |
| Hepatocellular injury | 41.30 | 21.08 | 48 | 15073 | 47545 | 79681722 |
| Ejection fraction decreased | 40.75 | 21.08 | 41 | 15080 | 34536 | 79694731 |
| Dermatitis exfoliative | 39.56 | 21.08 | 25 | 15096 | 10804 | 79718463 |
| Fall | 39.04 | 21.08 | 22 | 15099 | 487607 | 79241660 |
| Dysgeusia | 38.86 | 21.08 | 51 | 15070 | 57126 | 79672141 |
| Dizziness | 36.40 | 21.08 | 28 | 15093 | 526413 | 79202854 |
| Weight increased | 35.91 | 21.08 | 5 | 15116 | 277381 | 79451886 |
| Hepatotoxicity | 35.20 | 21.08 | 46 | 15075 | 51306 | 79677961 |
| Alopecia | 35.13 | 21.08 | 110 | 15011 | 231245 | 79498022 |
| Drug hypersensitivity | 35.12 | 21.08 | 7 | 15114 | 298909 | 79430358 |
| Gamma-glutamyltransferase increased | 34.45 | 21.08 | 47 | 15074 | 54633 | 79674634 |
| Myalgia | 33.65 | 21.08 | 94 | 15027 | 185547 | 79543720 |
| Acute kidney injury | 33.61 | 21.08 | 190 | 14931 | 519214 | 79210053 |
| Rash follicular | 33.30 | 21.08 | 7 | 15114 | 110 | 79729157 |
| Radiation necrosis | 33.11 | 21.08 | 9 | 15112 | 436 | 79728831 |
| Mass | 32.98 | 21.08 | 27 | 15094 | 17445 | 79711822 |
| Skin exfoliation | 32.67 | 21.08 | 46 | 15075 | 55054 | 79674213 |
| Panniculitis lobular | 32.36 | 21.08 | 6 | 15115 | 47 | 79729220 |
| Sarcoidosis | 32.35 | 21.08 | 20 | 15101 | 8315 | 79720952 |
| Dry skin | 32.07 | 21.08 | 51 | 15070 | 67944 | 79661323 |
| Serous retinopathy | 31.08 | 21.08 | 7 | 15114 | 154 | 79729113 |
| Dermatitis | 30.25 | 21.08 | 28 | 15093 | 21293 | 79707974 |
| Infusion related reaction | 30.15 | 21.08 | 4 | 15117 | 230233 | 79499034 |
| Blood creatinine increased | 29.57 | 21.08 | 80 | 15041 | 154977 | 79574290 |
| Drug eruption | 29.56 | 21.08 | 39 | 15082 | 43896 | 79685371 |
| Dermal cyst | 29.42 | 21.08 | 13 | 15108 | 2719 | 79726548 |
| Blood pressure increased | 29.35 | 21.08 | 3 | 15118 | 211357 | 79517910 |
| Renal failure | 28.18 | 21.08 | 93 | 15028 | 200875 | 79528392 |
| Skin mass | 27.92 | 21.08 | 18 | 15103 | 8045 | 79721222 |
| Rash papular | 27.70 | 21.08 | 27 | 15094 | 21889 | 79707378 |
| Nasopharyngitis | 27.70 | 21.08 | 7 | 15114 | 253874 | 79475393 |
| Malignant melanoma in situ | 27.48 | 21.08 | 12 | 15109 | 2440 | 79726827 |
| Intracranial tumour haemorrhage | 27.05 | 21.08 | 8 | 15113 | 527 | 79728740 |
| Product dose omission issue | 26.67 | 21.08 | 7 | 15114 | 247530 | 79481737 |
| Skin reaction | 26.55 | 21.08 | 23 | 15098 | 16045 | 79713222 |
| Palmar-plantar erythrodysaesthesia syndrome | 26.40 | 21.08 | 32 | 15089 | 33102 | 79696165 |
| Joint swelling | 26.15 | 21.08 | 11 | 15110 | 288635 | 79440632 |
| Metastases to meninges | 25.99 | 21.08 | 13 | 15108 | 3588 | 79725679 |
| Metastasis | 25.42 | 21.08 | 16 | 15105 | 6864 | 79722403 |
| Epidermal naevus syndrome | 25.27 | 21.08 | 4 | 15117 | 10 | 79729257 |
| BRAF gene mutation | 24.89 | 21.08 | 5 | 15116 | 62 | 79729205 |
| Toxicity to various agents | 24.83 | 21.08 | 26 | 15095 | 421514 | 79307753 |
| Transaminases increased | 24.66 | 21.08 | 39 | 15082 | 51704 | 79677563 |
| Milia | 23.88 | 21.08 | 5 | 15116 | 77 | 79729190 |
| Blood alkaline phosphatase increased | 23.73 | 21.08 | 43 | 15078 | 63621 | 79665646 |
| Vogt-Koyanagi-Harada disease | 23.12 | 21.08 | 6 | 15115 | 243 | 79729024 |
| Rash erythematous | 22.79 | 21.08 | 40 | 15081 | 57729 | 79671538 |
| Pancreatitis | 22.67 | 21.08 | 44 | 15077 | 68531 | 79660736 |
| Dysphagia | 22.26 | 21.08 | 62 | 15059 | 122074 | 79607193 |
| Dermatitis exfoliative generalised | 22.25 | 21.08 | 15 | 15106 | 7226 | 79722041 |
| Acantholysis | 22.23 | 21.08 | 4 | 15117 | 26 | 79729241 |
| Skin hypopigmentation | 22.17 | 21.08 | 8 | 15113 | 987 | 79728280 |
| Superficial spreading melanoma stage unspecified | 22.05 | 21.08 | 6 | 15115 | 292 | 79728975 |
| Abdominal discomfort | 22.00 | 21.08 | 10 | 15111 | 250717 | 79478550 |
| Rash morbilliform | 21.97 | 21.08 | 14 | 15107 | 6136 | 79723131 |
| General physical health deterioration | 21.39 | 21.08 | 106 | 15015 | 275132 | 79454135 |
| Eosinophilia | 21.36 | 21.08 | 34 | 15087 | 45311 | 79683956 |
| Neoplasm | 21.34 | 21.08 | 16 | 15105 | 9100 | 79720167 |
| Fatigue | 21.25 | 21.08 | 269 | 14852 | 929458 | 78799809 |
| Hepatitis | 21.23 | 21.08 | 38 | 15083 | 55689 | 79673578 |
| Recall phenomenon | 21.13 | 21.08 | 8 | 15113 | 1129 | 79728138 |
| Skin disorder | 21.11 | 21.08 | 29 | 15092 | 33914 | 79695353 |
None
| Source | Code | Description |
|---|---|---|
| ATC | L01EC01 | 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 | N0000182138 | Cytochrome P450 1A2 Inhibitors |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:75047 | BRAF inhibitors |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Erdheim-Chester Disease | indication | 699537002 | DOID:4329 |
| Malignant Melanoma with BRAF V600E Mutation | indication | 830150003 | |
| Hypocalcemia | contraindication | 5291005 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Torsades de pointes | contraindication | 31722008 | |
| Hypokalemia | contraindication | 43339004 | |
| Bradycardia | contraindication | 48867003 | |
| Acute nephropathy | contraindication | 58574008 | |
| Iritis | contraindication | 65074000 | DOID:1406 |
| Prolonged QT interval | contraindication | 111975006 | |
| Uveitis | contraindication | 128473001 | DOID:13141 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Decompensated chronic heart failure | contraindication | 424404003 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Retinal Blood Vessel Occlusions | contraindication |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.98 | acidic |
| pKa2 | 13.65 | acidic |
| pKa3 | 4.56 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 240MG | ZELBORAF | HOFFMANN LA ROCHE | N202429 | Aug. 17, 2011 | RX | TABLET | ORAL | 8470818 | Aug. 2, 2026 | TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAFV600E MUTATION AS DETECTED BY AN FDA APPROVED TEST |
| 240MG | ZELBORAF | HOFFMANN LA ROCHE | N202429 | Aug. 17, 2011 | RX | TABLET | ORAL | 8470818 | Aug. 2, 2026 | ZELBORAF IS INDICATED FOR THE TREATMENT OF PATIENTS WITH ERDHEIM-CHESTER DISEASE WITH BRAF V600 MUTATION |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 240MG | ZELBORAF | HOFFMANN LA ROCHE | N202429 | Aug. 17, 2011 | RX | TABLET | ORAL | Nov. 6, 2024 | TREATMENT OF PATIENTS WITH ERDHEIM-CHESTER DISEASE WITH BRAF V600 MUTATION |
| 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 | 7.68 | CHEMBL | CHEMBL | |||
| RAF proto-oncogene serine/threonine-protein kinase | Kinase | IC50 | 7.32 | CHEMBL | |||||
| Vascular endothelial growth factor receptor 2 | Kinase | IC50 | 6.44 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase kinase 5 | Kinase | Kd | 5.75 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 6.37 | CHEMBL | |||||
| TGF-beta receptor type-2 | Kinase | Kd | 5.47 | CHEMBL | |||||
| Protein-tyrosine kinase 6 | Kinase | Kd | 5.85 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase MLT | Kinase | IC50 | 7.64 | CHEMBL | |||||
| Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 6.13 | CHEMBL | |||||
| Serine/threonine-protein kinase A-Raf | Kinase | IC50 | 6.02 | CHEMBL | |||||
| GTPase KRas | Enzyme | IC50 | 4.78 | CHEMBL | |||||
| Ferrochelatase, mitochondrial | Enzyme | EC50 | 5.30 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 3 | Kinase | Kd | 5.68 | CHEMBL | |||||
| Aspartyl/asparaginyl beta-hydroxylase | Enzyme | IC50 | 4.98 | CHEMBL | |||||
| Serine/threonine-protein kinase B-raf | Kinase | IC50 | 7.52 | CHEMBL | |||||
| Dual specificity mitogen-activated protein kinase kinase 4 | Unclassified | Kd | 8.09 | CHEMBL |
| ID | Source |
|---|---|
| 4030980 | VUID |
| N0000183250 | NUI |
| D09996 | KEGG_DRUG |
| 4030980 | VANDF |
| C3192263 | UMLSCUI |
| CHEBI:63637 | CHEBI |
| 032 | PDB_CHEM_ID |
| CHEMBL1229517 | ChEMBL_ID |
| D000077484 | MESH_DESCRIPTOR_UI |
| DB08881 | DRUGBANK_ID |
| 5893 | IUPHAR_LIGAND_ID |
| 9286 | INN_ID |
| 207SMY3FQT | UNII |
| 42611257 | PUBCHEM_CID |
| 1147220 | RXNORM |
| 185260 | MMSL |
| 28057 | MMSL |
| d07798 | MMSL |
| 013887 | NDDF |
| 702805007 | SNOMEDCT_US |
| 703656005 | SNOMEDCT_US |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ZELBORAF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-090 | TABLET, FILM COATED | 240 mg | ORAL | NDA | 29 sections |
| ZELBORAF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-090 | TABLET, FILM COATED | 240 mg | ORAL | NDA | 29 sections |