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| Stem definition | Drug id | CAS RN |
|---|---|---|
| farnesyl transferase inhibitors | 5414 | 193275-84-2 |
None
| 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 |
| BA (Bioavailability) | 40 % |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,STK33,SYK,TEK,TTK | 37 | |||
| kinase-selectivity-class | AXL,PDK1 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 20, 2020 | FDA | EIGER BIOPHARMACEUTICALS INC | |
| July 18, 2022 | EMA | EIGERBIO EUROPE LIMITED |
None
None
None
None
| Source | Code | Description |
|---|---|---|
| ATC | A16AX20 | ALIMENTARY TRACT AND METABOLISM OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS Various alimentary tract and metabolism products |
| MeSH PA | D004791 | Enzyme Inhibitors |
| FDA MoA | N0000182140 | Cytochrome P450 2C19 Inhibitors |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000187062 | Cytochrome P450 2C8 Inhibitors |
| FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
| FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| FDA EPC | N0000193938 | Farnesyltransferase Inhibitor |
| FDA MoA | N0000193939 | Farnesyltransferase Inhibitors |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:64133 | EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hutchinson-Gilford syndrome | indication | 238870004 | DOID:3911 |
| Processingdeficient progeroid laminopathies | indication | ||
| Drug induction of cytochrome p450 CYP3A enzyme | contraindication | 423236002 | |
| Drug inhibition of cytochrome p450 CYP3A enzyme | contraindication | 423819001 | |
| Severe hepatic impairment | contraindication | 710067001 |
None
None
None
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 50MG | ZOKINVY | SENTYNL THERAPS INC | N213969 | Nov. 20, 2020 | RX | CAPSULE | ORAL | 7838531 | July 26, 2029 | REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) |
| 75MG | ZOKINVY | SENTYNL THERAPS INC | N213969 | Nov. 20, 2020 | RX | CAPSULE | ORAL | 7838531 | July 26, 2029 | REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 50MG | ZOKINVY | SENTYNL THERAPS INC | N213969 | Nov. 20, 2020 | RX | CAPSULE | ORAL | Nov. 20, 2027 | TREATMENT OF HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) AND PROGEROID LAMINOPATHIES |
| 75MG | ZOKINVY | SENTYNL THERAPS INC | N213969 | Nov. 20, 2020 | RX | CAPSULE | ORAL | Nov. 20, 2027 | TREATMENT OF HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) AND PROGEROID LAMINOPATHIES |
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Protein farnesyltransferase | Enzyme | INHIBITOR | IC50 | 8.72 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| GTPase HRas | Cytosolic other | INHIBITOR | IC50 | 8.72 | IUPHAR | ||||
| GTPase KRas | Enzyme | INHIBITOR | IC50 | 8.28 | IUPHAR | ||||
| GTPase NRas | Enzyme | INHIBITOR | IC50 | 8.55 | IUPHAR |
| ID | Source |
|---|---|
| D04768 | KEGG_DRUG |
| IOW153004F | UNII |
| C1257385 | UMLSCUI |
| CHEBI:47097 | CHEBI |
| 336 | PDB_CHEM_ID |
| CHEMBL298734 | ChEMBL_ID |
| 148195 | PUBCHEM_CID |
| DB06448 | DRUGBANK_ID |
| 8191 | INN_ID |
| C115354 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8024 | IUPHAR_LIGAND_ID |
| 1137365008 | SNOMEDCT_US |
| 1137617003 | SNOMEDCT_US |
| 4041665 | VANDF |
| 341166 | MMSL |
| 39043 | MMSL |
| d09683 | MMSL |
| 018565 | NDDF |
| 2467553 | RXNORM |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Zokinvy | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42358-450 | CAPSULE | 50 mg | ORAL | NDA | 28 sections |
| Zokinvy | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42358-475 | CAPSULE | 75 mg | ORAL | NDA | 28 sections |
| Zokinvy | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73079-050 | CAPSULE | 50 mg | ORAL | NDA | 30 sections |
| Zokinvy | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73079-075 | CAPSULE | 75 mg | ORAL | NDA | 30 sections |