Stem definition | Drug id | CAS RN |
---|---|---|
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors | 5289 | 1269440-17-6 |
Dose | Unit | Route |
---|---|---|
0.45 | g | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
June 27, 2018 | FDA | ARRAY BIOPHARMA INC | |
Jan. 8, 2019 | PMDA | Ono Pharmaceutical Co., Ltd. |
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 |
---|---|---|---|---|---|---|
Serous retinal detachment | 429.38 | 29.75 | 57 | 2220 | 224 | 56289566 |
Neoplasm progression | 153.12 | 29.75 | 55 | 2222 | 31961 | 56257829 |
Serous retinopathy | 105.30 | 29.75 | 13 | 2264 | 23 | 56289767 |
Death | 80.73 | 29.75 | 83 | 2194 | 341343 | 55948447 |
Retinal detachment | 70.50 | 29.75 | 20 | 2257 | 5421 | 56284369 |
Off label use | 65.52 | 29.75 | 95 | 2182 | 556085 | 55733705 |
Second primary malignancy | 56.10 | 29.75 | 18 | 2259 | 7384 | 56282406 |
Macular detachment | 45.72 | 29.75 | 7 | 2270 | 86 | 56289704 |
Hospice care | 42.65 | 29.75 | 14 | 2263 | 6166 | 56283624 |
Pyrexia | 41.24 | 29.75 | 66 | 2211 | 418707 | 55871083 |
Hepatic function abnormal | 40.13 | 29.75 | 22 | 2255 | 34536 | 56255254 |
Disease progression | 39.04 | 29.75 | 33 | 2244 | 105140 | 56184650 |
Colitis | 36.23 | 29.75 | 22 | 2255 | 41789 | 56248001 |
Intestinal obstruction | 33.00 | 29.75 | 18 | 2259 | 27953 | 56261837 |
Nausea | 31.52 | 29.75 | 84 | 2193 | 764094 | 55525696 |
Decreased appetite | 30.87 | 29.75 | 41 | 2236 | 219190 | 56070600 |
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 |
---|---|---|---|---|---|---|
Serous retinal detachment | 414.02 | 33.22 | 65 | 2369 | 476 | 31694434 |
Neoplasm progression | 179.96 | 33.22 | 65 | 2369 | 20207 | 31674703 |
Serous retinopathy | 105.40 | 33.22 | 16 | 2418 | 90 | 31694820 |
Death | 44.60 | 33.22 | 90 | 2344 | 360479 | 31334431 |
Disease progression | 44.45 | 33.22 | 44 | 2390 | 90420 | 31604490 |
Second primary malignancy | 38.81 | 33.22 | 16 | 2418 | 7016 | 31687894 |
Pyrexia | 35.28 | 33.22 | 74 | 2360 | 303766 | 31391144 |
Nausea | 34.60 | 33.22 | 74 | 2360 | 307873 | 31387037 |
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 |
---|---|---|---|---|---|---|
Serous retinal detachment | 791.65 | 29.06 | 119 | 4539 | 753 | 70923033 |
Neoplasm progression | 298.80 | 29.06 | 112 | 4546 | 45116 | 70878670 |
Serous retinopathy | 203.92 | 29.06 | 29 | 4629 | 115 | 70923671 |
Death | 131.86 | 29.06 | 164 | 4494 | 509897 | 70413889 |
Second primary malignancy | 84.80 | 29.06 | 32 | 4626 | 13019 | 70910767 |
Off label use | 78.94 | 29.06 | 159 | 4499 | 742901 | 70180885 |
Retinal detachment | 78.47 | 29.06 | 27 | 4631 | 8440 | 70915346 |
Pyrexia | 60.86 | 29.06 | 127 | 4531 | 606825 | 70316961 |
Hospice care | 56.50 | 29.06 | 21 | 4637 | 8184 | 70915602 |
Disease progression | 56.35 | 29.06 | 60 | 4598 | 156612 | 70767174 |
Uveitis | 53.92 | 29.06 | 24 | 4634 | 14821 | 70908965 |
Nausea | 52.83 | 29.06 | 148 | 4510 | 851940 | 70071846 |
Hepatic function abnormal | 52.30 | 29.06 | 40 | 4618 | 67956 | 70855830 |
Vision blurred | 50.32 | 29.06 | 45 | 4613 | 94939 | 70828847 |
Macular detachment | 49.52 | 29.06 | 9 | 4649 | 197 | 70923589 |
Blood creatine phosphokinase increased | 47.03 | 29.06 | 36 | 4622 | 61227 | 70862559 |
Diarrhoea | 43.58 | 29.06 | 131 | 4527 | 783210 | 70140576 |
Colitis | 41.47 | 29.06 | 34 | 4624 | 63780 | 70860006 |
Dermatitis acneiform | 40.83 | 29.06 | 17 | 4641 | 8928 | 70914858 |
Retinopathy | 35.69 | 29.06 | 12 | 4646 | 3494 | 70920292 |
Decreased appetite | 32.99 | 29.06 | 66 | 4592 | 304714 | 70619072 |
Lipase increased | 32.17 | 29.06 | 17 | 4641 | 15229 | 70908557 |
Amylase increased | 29.24 | 29.06 | 14 | 4644 | 10194 | 70913592 |
None
Source | Code | Description |
---|---|---|
ATC | L01EC03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS B-Raf serine-threonine kinase (BRAF) inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Metastatic malignant melanoma | indication | 443493003 | |
Unresectable malignant melanoma with BRAF gene mutation | indication | 830150003 | |
BRAF mutation-positive colorectal cancer | indication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.37 | acidic |
pKa2 | 13.42 | acidic |
pKa3 | 3.69 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 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, 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 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, 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 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, 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 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, 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 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 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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
50MG | BRAFTOVI | ARRAY BIOPHARMA INC | N210496 | June 27, 2018 | DISCN | CAPSULE | ORAL | April 8, 2023 | ENCORAFENIB, IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULTPATIENTS WITH METASTATIC COLORECTAL CANCER 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 | April 8, 2023 | ENCORAFENIB, IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULTPATIENTS WITH METASTATIC COLORECTAL CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY |
50MG | BRAFTOVI | ARRAY BIOPHARMA INC | N210496 | June 27, 2018 | DISCN | CAPSULE | ORAL | June 27, 2023 | NEW CHEMICAL ENTITY |
75MG | BRAFTOVI | ARRAY BIOPHARMA INC | N210496 | June 27, 2018 | RX | CAPSULE | ORAL | June 27, 2023 | NEW CHEMICAL ENTITY |
50MG | BRAFTOVI | ARRAY BIOPHARMA INC | N210496 | June 27, 2018 | DISCN | CAPSULE | ORAL | June 27, 2025 | ENCORAFENIB IS 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 | June 27, 2025 | ENCORAFENIB IS 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 |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
8L7891MRB6 | UNII |
C4079208 | UMLSCUI |
CHEMBL3301612 | ChEMBL_ID |
50922675 | PUBCHEM_CID |
DB11718 | DRUGBANK_ID |
D11053 | KEGG_DRUG |
9816 | INN_ID |
7908 | IUPHAR_LIGAND_ID |
283907 | MMSL |
34462 | MMSL |
d08817 | MMSL |
017615 | NDDF |
772091004 | SNOMEDCT_US |
772201002 | SNOMEDCT_US |
4037644 | VANDF |
C000601108 | MESH_SUPPLEMENTAL_RECORD_UI |
2049106 | RXNORM |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
BRAFTOVI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70255-025 | CAPSULE | 75 mg | ORAL | NDA | 32 sections |
BRAFTOVI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70255-025 | CAPSULE | 75 mg | ORAL | NDA | 32 sections |
BRAFTOVI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70255-050 | CAPSULE | 50 mg | ORAL | EXPORT ONLY | 1 sections |