trifluridine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
uridine derivatives used as antiviral agents and as antineoplastics	2743	70-00-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: trifluridine trifluorothymidine 5-Trifluorothymidine	An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557) Molecular weight: 296.20 Formula: C10H11F3N2O5 CLOGP: -0.41 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 99.10 ALOGS: -1.65 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

trifluridine
trifluorothymidine
5-Trifluorothymidine

An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557)

Molecular weight: 296.20
Formula: C10H11F3N2O5
CLOGP: -0.41
LIPINSKI: 0
HAC: 7
HDO: 3
TPSA: 99.10
ALOGS: -1.65
ROTB: 3

Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
April 10, 1980	FDA	MONARCH PHARMS
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:

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Source	Code	Description
ATC	L01BC59	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Pyrimidine analogues
ATC	S01AD02	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Antivirals
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:63720	dTMP synthase inhibitors
FDA EPC	N0000175466	Nucleoside Analog Antiviral
FDA EPC	N0000175595	Nucleoside Metabolic Inhibitor
FDA EXT	N0000175459	Nucleoside Analog
FDA MoA	N0000000233	Nucleic Acid Synthesis Inhibitors

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

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Disease	Relation	SNOMED_ID	DOID
Herpes simplex keratitis	indication	9389005
Herpes simplex keratoconjunctivitis	indication	72321008
Malignant tumor of stomach	indication	363349007	DOID:10534
Malignant tumor of colon	indication	363406005	DOID:219

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.95	acidic
pKa2	13.02	acidic
pKa3	13.7	acidic

Orange Book patent data (new drug applications)

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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

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Orange Book exclusivity data (new drug applications)

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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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Thymidine kinase	Kinase		A3RLP8_CHV1		IC50	5.70		CHEMBL
Thymidylate kinase	Kinase		KTHY_MYCTU		Ki	4.01		CHEMBL

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External reference:

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ID	Source
003015	NDDF
10803	RXNORM
373512003	SNOMEDCT_US
4018780	VUID
4018780	VANDF
4146	INN_ID
5627	MMSL
58892008	SNOMEDCT_US
6256	PUBCHEM_CID
6442	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
LONSURF	HUMAN PRESCRIPTION DRUG LABEL	2	64842-1020	TABLET, FILM COATED	20 mg	ORAL	NDA	27 sections
LONSURF	HUMAN PRESCRIPTION DRUG LABEL	2	64842-1020	TABLET, FILM COATED	20 mg	ORAL	NDA	27 sections
LONSURF	HUMAN PRESCRIPTION DRUG LABEL	2	64842-1025	TABLET, FILM COATED	15 mg	ORAL	NDA	27 sections
LONSURF	HUMAN PRESCRIPTION DRUG LABEL	2	64842-1025	TABLET, FILM COATED	15 mg	ORAL	NDA	27 sections
Trifluridine	HUMAN PRESCRIPTION DRUG LABEL	1	50383-955	SOLUTION/ DROPS	10 mg	OPHTHALMIC	ANDA	21 sections
Trifluridine	HUMAN PRESCRIPTION DRUG LABEL	1	61314-044	SOLUTION	10 mg	OPHTHALMIC	ANDA	18 sections

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