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borofalan (10B) 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5422 | 80994-59-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Borofalan is a boron compound, namely phenylalanine labeled with 10B (an isotope of boron). Phenylalanine is an amino acid essential for the growth of tumor cells. It has been suggested that the compound accumulatesin tumor cells, mediated by L-type amino acid transporter-1 (LAT-1), an amino acid transporter highly expressed in multiple types of carcinomas including head and neck cancer. Borofalan alone does not inhibit tumor growth, whereas upon irradiation of neutron beams from outside the body, 10B atoms incorporated in tumorcells capture neutrons, resulting in the release of alpha rays and lithium nuclei generated by nuclear reaction, exhibiting a tumor growth-inhibitory effect.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -2.357 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.710 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.288 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.099 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 73.720 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 79.510 | % | High | 1 |
| herg | hERG pIC50 | 4.848 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.084 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.266 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 82.590 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GRK3,GSK3B,ITK,JAK2,JAK3,KDR,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 | 45 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,GRK2,MAP2K6,TEK,TGFBR1 | 7 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.519 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.649 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 0.982 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 94.230 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.211 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 87.550 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.009 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 0.897 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.570 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 86.800 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 796.159 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 25, 2020 | PMDA | Stella Pharma |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Neoplasm of head and neck | indication | 255055008 | DOID:11934 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| L-type amino acid transporter 1 | Transporter | SUBSTRATE | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| D11272 | KEGG_DRUG |
| C5419351 | UMLSCUI |
| 25033700 | PUBCHEM_CID |
| 57659839UA | UNII |
| UID84303EL | UNII |
Pharmaceutical products:
None