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avapritinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5379 | 1703793-34-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Avapritinib is a tyrosine kinase inhibitor that targets PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC50s) less than 25 nM. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.632 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.954 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 21.979 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.715 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 2.430 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 10.890 | % | High | 1 |
| herg | hERG pIC50 | 5.393 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.600 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 9.441 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.760 | % | High | 1 |
| kinase-safety-class | AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK7,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,NTRK1,NTRK2,NTRK3,NUAK1,PAK4,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PRKAA1,PRKAA2,PRKCD,PRKDC,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 | 109 | |||
| kinase-selectivity-class | ABL2,ACVR2B,ACVRL1,AKT3,AURKB,AURKC,AXL,BLK,BTK,CAMK2D,CHEK1,CLK2,CLK4,CSF1R,EGFR,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,IRAK3,KDR,KIT,LCK,LYN,MAP3K11,MAP3K7,MAP4K1,MAP4K3,MAP4K4,MAP4K5,MARK1,MARK2,MARK3,MARK4,MET,MINK1,MKNK2,NTRK1,NTRK3,NUAK1,PDGFRB,PDK1,RET,RIPK3,SIK2,SIK3,SRC,TGFBR1,TNIK,YES1 | 52 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 10.617 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.656 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.230 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 25.235 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 3.650 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.042 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 5.957 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 12.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.410 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 2.178 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 24, 2020 | EMA | Blueprint Medicines (Netherlands) B.V. | |
| Jan. 9, 2020 | FDA | BLUEPRINT MEDICINES |
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 |
|---|---|---|---|---|---|---|
| Off label use | 147.26 | 31.12 | 138 | 1584 | 1102114 | 89524611 |
| Periorbital oedema | 101.69 | 31.12 | 24 | 1698 | 6775 | 90619950 |
| Disease progression | 86.25 | 31.12 | 47 | 1675 | 156568 | 90470157 |
| Hair colour changes | 77.42 | 31.12 | 17 | 1705 | 3477 | 90623248 |
| Face oedema | 76.44 | 31.12 | 25 | 1697 | 23293 | 90603432 |
| Periorbital swelling | 61.70 | 31.12 | 15 | 1707 | 4783 | 90621942 |
| Tryptase increased | 58.37 | 31.12 | 10 | 1712 | 557 | 90626168 |
| Cognitive disorder | 35.80 | 31.12 | 20 | 1702 | 69387 | 90557338 |
| Persistent postural-perceptual dizziness | 33.05 | 31.12 | 4 | 1718 | 16 | 90626709 |
| Swelling face | 32.85 | 31.12 | 20 | 1702 | 81332 | 90545393 |
| Eye swelling | 31.72 | 31.12 | 14 | 1708 | 29372 | 90597353 |
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 |
|---|---|---|---|---|---|---|
| Off label use | 145.65 | 38.89 | 134 | 1205 | 638201 | 41981795 |
| Hair colour changes | 105.02 | 38.89 | 22 | 1317 | 2180 | 42617816 |
| Periorbital oedema | 64.09 | 38.89 | 17 | 1322 | 4640 | 42615356 |
| Memory impairment | 45.86 | 38.89 | 25 | 1314 | 50197 | 42569799 |
| Tryptase increased | 45.22 | 38.89 | 8 | 1331 | 322 | 42619674 |
| Face oedema | 42.41 | 38.89 | 16 | 1323 | 13650 | 42606346 |
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 |
|---|---|---|---|---|---|---|
| Off label use | 162.78 | 29.87 | 178 | 2202 | 1500007 | 109086912 |
| Hair colour changes | 118.52 | 29.87 | 26 | 2354 | 4675 | 110582244 |
| Face oedema | 94.15 | 29.87 | 33 | 2347 | 33436 | 110553483 |
| Periorbital oedema | 89.02 | 29.87 | 24 | 2356 | 10168 | 110576751 |
| Periorbital swelling | 72.61 | 29.87 | 18 | 2362 | 5487 | 110581432 |
| Disease progression | 66.09 | 29.87 | 49 | 2331 | 243985 | 110342934 |
| Tryptase increased | 64.64 | 29.87 | 12 | 2368 | 931 | 110585988 |
| Lacrimation increased | 42.07 | 29.87 | 18 | 2362 | 30932 | 110555987 |
| Eyelid oedema | 38.90 | 29.87 | 14 | 2366 | 15248 | 110571671 |
| Swelling face | 37.89 | 29.87 | 24 | 2356 | 92297 | 110494622 |
| Eye swelling | 34.57 | 29.87 | 16 | 2364 | 33032 | 110553887 |
| Nausea | 34.20 | 29.87 | 79 | 2301 | 1235611 | 109351308 |
| Memory impairment | 33.09 | 29.87 | 30 | 2350 | 196914 | 110390005 |
| Myelosuppression | 32.54 | 29.87 | 22 | 2358 | 94318 | 110492601 |
| Cognitive disorder | 31.60 | 29.87 | 21 | 2359 | 87490 | 110499429 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EX18 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
| FDA MoA | N0000020001 | Tyrosine Kinase Inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000191423 | Multidrug and Toxin Extrusion Transporter 1 Inhibitors |
| FDA MoA | N0000193845 | Bile Salt Export Pump Inhibitors |
| FDA MoA | N0000193932 | Multidrug and Toxin Extrusion Transporter 2 K Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01EX Other protein kinase inhibitors 21 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Systemic mast cell disease | indication | 397016004 | DOID:349 |
| Gastrointestinal stromal tumor | indication | 420120006 | DOID:9253 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.82 | Basic |
| pKa2 | 6.22 | Basic |
| pKa3 | 1.64 | Basic |
| pKa4 | 1.05 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 11827642 | Oct. 15, 2034 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9200002 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9944651 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 9994575 | Oct. 15, 2034 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 11999744 | April 10, 2040 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 11999744 | April 10, 2040 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 11999744 | April 10, 2040 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 11999744 | April 10, 2040 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 12252494 | April 10, 2040 | TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | 11999744 | April 10, 2040 | TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 12060354 | March 8, 2042 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 12060354 | March 8, 2042 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | 12060354 | March 8, 2042 | TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | May 22, 2026 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | Jan. 9, 2027 | INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | Jan. 9, 2027 | INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | Jan. 9, 2027 | INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | Jan. 9, 2027 | INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | Jan. 9, 2027 | INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | June 16, 2028 | FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | June 16, 2028 | FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | June 16, 2028 | FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | June 16, 2028 | FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | June 16, 2028 | FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL) |
| 100MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | May 22, 2030 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 200MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | May 22, 2030 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 25MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | May 22, 2030 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 300MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | Jan. 9, 2020 | RX | TABLET | ORAL | May 22, 2030 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
| 50MG | AYVAKIT | BLUEPRINT MEDICINES | N212608 | June 16, 2021 | RX | TABLET | ORAL | May 22, 2030 | TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM) |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mast/stem cell growth factor receptor Kit | Kinase | INHIBITOR | IC50 | 9.57 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Platelet-derived growth factor receptor alpha | Kinase | INHIBITOR | IC50 | 9.62 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 8.82 | CHEMBL | |||||
| Mast/stem cell growth factor receptor Kit | Kinase | INHIBITOR | IC50 | 7.66 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 513P80B4YJ | UNII |
| 4039082 | VANDF |
| C4743552 | UMLSCUI |
| CHEBI:756628 | CHEBI |
| 9JI | PDB_CHEM_ID |
| CHEMBL4204794 | ChEMBL_ID |
| 118023034 | PUBCHEM_CID |
| DB15233 | DRUGBANK_ID |
| D000099289 | MESH_DESCRIPTOR_UI |
| 10613 | INN_ID |
| D11279 | KEGG_DRUG |
| 10368 | IUPHAR_LIGAND_ID |
| 838409003 | SNOMEDCT_US |
| 838462005 | SNOMEDCT_US |
| 329235 | MMSL |
| 37922 | MMSL |
| d09480 | MMSL |
| 018251 | NDDF |
| 2272107 | RXNORM |
| 513P80B4YJ | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Ayvakit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72064-110 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 31 sections |
| Ayvakit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72064-120 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 31 sections |
| Ayvakit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72064-125 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 31 sections |
| Ayvakit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72064-130 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 31 sections |
| Ayvakit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72064-150 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 31 sections |