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
Molfile Inchi Smiles Synonyms: tipiracil tipiracil hydrochloride tipiracil HCl	tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase Molecular weight: 242.66 Formula: C9H11ClN4O2 CLOGP: -0.30 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 85.29 ALOGS: -2.52 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tipiracil
tipiracil hydrochloride
tipiracil HCl

tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase

Molecular weight: 242.66
Formula: C9H11ClN4O2
CLOGP: -0.30
LIPINSKI: 0
HAC: 6
HDO: 3
TPSA: 85.29
ALOGS: -2.52
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
March 24, 2014	PMDA	Taiho Pharmaceutical Co., Ltd.
Sept. 22, 2015	FDA	TAIHO ONCOLOGY INC

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:

Show entries

Search:

Source	Code	Description
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:90878	pyrimidine deoxynucleoside phosphorylase inhibitors
FDA EPC	N0000191870	Thymidine Phosphorylase Inhibitor
FDA MoA	N0000191869	Thymidine Phosphorylase Inhibitors

Showing 1 to 4 of 4 entries

Previous1Next

Drug Use | Suggest Off label Use Form| |View source of the data|

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Malignant tumor of stomach	indication	363349007	DOID:10534
Malignant tumor of colon	indication	363406005	DOID:219

Showing 1 to 2 of 2 entries

Previous1Next

🐶 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)

Show entries

Search:

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 APPROPRIATE, 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 METASTATIC COLORECTAL CANCER ALONE OR WITH BEVACIZUMAB IN PATIENTS 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	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	9943537	Sept. 5, 2034	TREATMENT OF METASTATIC COLORECTAL CANCER WITH BEVACIZUMAB IN PATIENTS 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	10456399	Feb. 3, 2037	TREATMENT OF METASTATIC COLORECTAL CANCER ALONE OR WITH BEVACIZUMAB IN SEVERELY RENALLY IMPAIRED PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN THERAPY, AN ANTI-VEGF BIOLOGIC, AND IF RAS WILD-TYPE, ANTI-EGFR THERAPY
EQ 6.14MG BASE;15MG	LONSURF	TAIHO ONCOLOGY	N207981	Sept. 22, 2015	RX	TABLET	ORAL	10456399	Feb. 3, 2037	TREATMENT OF METASTATIC GASTRIC OR GJA IN SEVERELY RENALLY IMPAIRED PATIENTS TREATED WITH AT LEAST TWO LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, A TAXANE OR IRINOTECAN, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY
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 6.14MG BASE;15MG	LONSURF	TAIHO ONCOLOGY	N207981	Sept. 22, 2015	RX	TABLET	ORAL	10960004	Feb. 3, 2037	TREATMENT OF METASTATIC COLORECTAL CANCER ALONE OR WITH BEVACIZUMAB IN SEVERELY RENALLY IMPAIRED PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN THERAPY, AN ANTI-VEGF BIOLOGIC, AND IF RAS WILD-TYPE, ANTI-EGFR THERAPY
EQ 6.14MG BASE;15MG	LONSURF	TAIHO ONCOLOGY	N207981	Sept. 22, 2015	RX	TABLET	ORAL	10960004	Feb. 3, 2037	TREATMENT OF METASTATIC GASTRIC OR GJA IN SEVERELY RENALLY IMPAIRED PATIENTS TREATED WITH AT LEAST TWO LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, A TAXANE OR IRINOTECAN, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY

Showing 1 to 10 of 20 entries

Previous1 2Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

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, 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

Showing 1 to 2 of 2 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Thymidine phosphorylase	Enzyme	P19971	TYPH_HUMAN	INHIBITOR	IC50	7.70		SCIENTIFIC LITERATURE	DRUG LABEL
Thymidine phosphorylase	Enzyme		TYPH_ECOLI		IC50	7.70		CHEMBL

Showing 1 to 2 of 2 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
016454	NDDF
016455	NDDF
1670303	RXNORM
183204-72-0	SECONDARY_CAS_RN
31200	MMSL
4034880	VANDF
6323266	PUBCHEM_CID
724029008	SNOMEDCT_US
724030003	SNOMEDCT_US
8696	IUPHAR_LIGAND_ID

Showing 1 to 10 of 21 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

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	64842-1020	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
LONSURF	HUMAN PRESCRIPTION DRUG LABEL	2	64842-1025	TABLET, FILM COATED	6.14 mg	ORAL	NDA	27 sections

Showing 1 to 4 of 4 entries

Previous1Next