tipiracil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| uracil type antineoplastics | 4893 | 183204-74-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 22, 2015 | FDA | TAIHO ONCOLOGY INC | |
| March 24, 2014 | PMDA | Taiho Pharmaceutical Co., Ltd. |
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:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000191869 | Thymidine Phosphorylase Inhibitors |
| FDA EPC | N0000191870 | Thymidine Phosphorylase Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:90878 | pyrimidine deoxynucleoside phosphorylase inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant tumor of stomach | indication | 363349007 | DOID:10534 |
| Malignant tumor of colon | indication | 363406005 | DOID:219 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.78 | acidic |
| pKa2 | 9.98 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF ADULTS WITH METASTATIC GASTRIC OR GJA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, EITHER A TAXANE OR IRINOTECAN, AND IF APPROPIATE, HER2/NEU-TARGETED THERAPY |
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF ADULTS WITH METASTATIC GASTRIC OR GJA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, EITHER A TAXANE OR IRINOTECAN, AND IF APPROPIATE, HER2/NEU-TARGETED THERAPY |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY |
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10456399 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10960004 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10456399 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10960004 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2022 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2022 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
| EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2026 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
| EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2026 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Thymidine phosphorylase | Enzyme | INHIBITOR | IC50 | 7.70 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Thymidine phosphorylase | Enzyme | IC50 | 7.70 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| NGO10K751P | UNII |
| D10467 | KEGG_DRUG |
| 183204-72-0 | SECONDARY_CAS_RN |
| 4034880 | VANDF |
| C4056441 | UMLSCUI |
| CHEBI:90879 | CHEBI |
| CMU | PDB_CHEM_ID |
| CHEMBL235668 | ChEMBL_ID |
| 6323266 | PUBCHEM_CID |
| DB09343 | DRUGBANK_ID |
| CHEMBL65375 | ChEMBL_ID |
| 9500 | INN_ID |
| C000613754 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8696 | IUPHAR_LIGAND_ID |
| 1670303 | RXNORM |
| 31200 | MMSL |
| d08381 | MMSL |
| 016454 | NDDF |
| 016455 | NDDF |
| 724029008 | SNOMEDCT_US |
| 724030003 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| LONSURF | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-1020 | TABLET, FILM COATED | 8.19 mg | ORAL | NDA | 27 sections |
| LONSURF | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-1025 | TABLET, FILM COATED | 6.14 mg | ORAL | NDA | 27 sections |