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fruquintinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5750 | 1194506-26-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Fruquintinib is a small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 with IC50 values of 33, 35, and 0.5 nM, respectively. In vitro studies showed fruquintinib inhibited VEGF-mediated endothelial cell proliferation and tubular formation. In vitro and in vivo studies showed fruquintinib inhibited VEGF-induced VEGFR-2 phosphorylation. In vivo studies showed fruquintinib inhibited tumor growth in a tumor xenograft mouse model of colon cancer.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3.75 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.585 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.826 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 45.604 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.214 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 14.040 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 38.630 | % | High | 1 |
| herg | hERG pIC50 | 4.364 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.107 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.767 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 5.150 | % | High | 1 |
| kinase-safety-class | ABL1,ABL2,ACVR2B,ACVRL1,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT1,FLT3,FLT4,KDR,KIT,LCK,LYN,MAP3K21,MAPK7,NTRK1,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC,PTK6,RET,RIPK3,SRC,SYK,TTK,YES1 | 43 | |||
| kinase-selectivity-class | ACVR2B,AURKA,AXL,BLK,BRAF,CSF1R,CSK,DDR1,EGFR,ERBB2,FLT1,FLT4,IRAK3,KDR,KIT,LYN,PDGFRB,PDK4,PLK4,RIPK3 | 20 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.289 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.483 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 7.440 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.561 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 13.650 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.963 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 64.430 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 4.780 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 15.596 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 8, 2023 | FDA | TAKEDA PHARMS USA |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 258.83 | 38.36 | 74 | 1372 | 53517 | 90573484 |
| Death | 191.34 | 38.36 | 107 | 1339 | 456444 | 90170557 |
| Palmar-plantar erythrodysaesthesia syndrome | 109.76 | 38.36 | 33 | 1413 | 27990 | 90599011 |
| Proteinuria | 106.84 | 38.36 | 31 | 1415 | 23260 | 90603741 |
| Blood pressure increased | 73.14 | 38.36 | 43 | 1403 | 197174 | 90429827 |
| Hypertension | 66.23 | 38.36 | 56 | 1390 | 457476 | 90169525 |
| Hypothyroidism | 44.20 | 38.36 | 20 | 1426 | 53107 | 90573894 |
| Nephrotic syndrome | 43.72 | 38.36 | 12 | 1434 | 7327 | 90619674 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 266.02 | 35.16 | 89 | 1724 | 40372 | 42579150 |
| Death | 132.69 | 35.16 | 128 | 1685 | 471057 | 42148465 |
| Palmar-plantar erythrodysaesthesia syndrome | 125.82 | 35.16 | 43 | 1770 | 20539 | 42598983 |
| Proteinuria | 117.38 | 35.16 | 42 | 1771 | 22941 | 42596581 |
| Hypertension | 82.41 | 35.16 | 63 | 1750 | 167141 | 42452381 |
| Dysphonia | 80.92 | 35.16 | 34 | 1779 | 28416 | 42591106 |
| Decreased appetite | 62.29 | 35.16 | 57 | 1756 | 193080 | 42426442 |
| Metastases to liver | 41.37 | 35.16 | 18 | 1795 | 16308 | 42603214 |
| Asthenia | 39.91 | 35.16 | 54 | 1759 | 280739 | 42338783 |
| Fatigue | 35.71 | 35.16 | 65 | 1748 | 435576 | 42183946 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 549.81 | 36.34 | 164 | 2425 | 94176 | 110492534 |
| Proteinuria | 233.83 | 36.34 | 70 | 2519 | 39948 | 110546762 |
| Palmar-plantar erythrodysaesthesia syndrome | 210.72 | 36.34 | 65 | 2524 | 40960 | 110545750 |
| Death | 145.79 | 36.34 | 124 | 2465 | 698745 | 109887965 |
| Hypertension | 115.31 | 36.34 | 95 | 2494 | 509989 | 110076721 |
| Nephrotic syndrome | 92.90 | 36.34 | 27 | 2562 | 13804 | 110572906 |
| Decreased appetite | 78.03 | 36.34 | 74 | 2515 | 475772 | 110110938 |
| Hypothyroidism | 75.70 | 36.34 | 36 | 2553 | 72863 | 110513847 |
| Blood pressure increased | 64.17 | 36.34 | 51 | 2538 | 258322 | 110328388 |
| Dysphonia | 59.56 | 36.34 | 31 | 2558 | 75898 | 110510812 |
| Platelet count decreased | 58.30 | 36.34 | 46 | 2543 | 230397 | 110356313 |
| Renal impairment | 48.46 | 36.34 | 38 | 2551 | 188407 | 110398303 |
| White blood cell count decreased | 38.05 | 36.34 | 36 | 2553 | 229354 | 110357356 |
| Asthenia | 36.67 | 36.34 | 61 | 2528 | 688938 | 109897772 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EK04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors |
| MeSH PA | D000092004 | Tyrosine Kinase Inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D047428 | Protein Kinase Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:62434 | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| CHEBI has role | CHEBI:65207 | vascular endothelial growth factor receptor antagonist |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
L01EK Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Metastatic colorectal cancer (mCRC) | indication | 781076008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 1MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 8212033 | May 9, 2028 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
| 5MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 8212033 | May 9, 2028 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
| 1MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 10519142 | Sept. 7, 2035 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
| 1MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 11046674 | Sept. 7, 2035 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
| 5MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 10519142 | Sept. 7, 2035 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
| 5MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | 11046674 | Sept. 7, 2035 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 1MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | Nov. 8, 2028 | NEW CHEMICAL ENTITY |
| 5MG | FRUZAQLA | TAKEDA PHARMS USA | N217564 | Nov. 8, 2023 | RX | CAPSULE | ORAL | Nov. 8, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Vascular endothelial growth factor receptor 1 | Kinase | INHIBITOR | IC50 | 7.48 | DRUG LABEL | DRUG LABEL | |||
| Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 7.46 | DRUG LABEL | DRUG LABEL | |||
| Vascular endothelial growth factor receptor 3 | Kinase | INHIBITOR | IC50 | 9.30 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229221 | CHEBI |
| CHEMBL4303214 | ChEMBL_ID |
| C000591844 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9428 | IUPHAR_LIGAND_ID |
| DB11679 | DRUGBANK_ID |
| 1363353001 | SNOMEDCT_US |
| 4042767 | VANDF |
| C3640966 | UMLSCUI |
| 10348 | INN_ID |
| 44480399 | PUBCHEM_CID |
| 374215 | MMSL |
| 42177 | MMSL |
| d10132 | MMSL |
| 018657 | NDDF |
| 49DXG3M5ZW | UNII |
| 2670179 | RXNORM |
| D11977 | KEGG_DRUG |
| 49DXG3M5ZW | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Fruzaqla | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63020-210 | CAPSULE | 1 mg | ORAL | NDA | 31 sections |
| Fruzaqla | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63020-225 | CAPSULE | 5 mg | ORAL | NDA | 31 sections |