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Tipiracil hydrochloride

Tipiracil hydrochloride structure

CAS No:
183204-72-0
Formula:
C9H11ClN4O2.ClH
Chemical Name:
Tipiracil hydrochloride
Synonyms:
2,4(1H,3H)-Pyrimidinedione,5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-,hydrochloride (1:1);2,4(1H,3H)-Pyrimidinedione,5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-,monohydrochloride;TPI hydrochloride;TAS 1-462;Tipiracil hydrochloride;5-Chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride
Categories:
Chemical Reagents > Organic Reagents

Description

ChEBI: A hydrochloride obtained by combining tipiracil with one equivalent of hydrochloric acid. Used in combination with trifluridine, a nucleoside metabolic inhibitor, for treatment of advanced/relapsed unresectable colorectal cancer.

Tipiracil hydrochloride is a hydrochloride obtained by combining tipiracil with one equivalent of hydrochloric acid. Used in combination with trifluridine, a nucleoside metabolic inhibitor, for treatment of advanced/relapsed unresectable colorectal cancer. It has a role as an antineoplastic agent and an EC 2.4.2.4 (thymidine phosphorylase) inhibitor. It is a hydrochloride and an iminium salt. It contains a tipiracil(1+).

Tipiracil hydrochloride Basic Attributes

Molecular Weight：

279.12318

Exact Mass：

278.033722

UNII：

4H59KLQ0A4

ATC Code：

L01BC

Characteristics

PSA：

85.3

XLogP3：

1.95390

Melting Point：

245 °C (decomp)

Safety Information

Transport codes：

NONH for all modes of transport

Precautionary statement(s)：

P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, P501

Hazard Statements：

H315

GHS Classification：

|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 2 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Metastatic colorectal cancerLonsurf is indicated as monotherapy for the treatment of adult patients with metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies including fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapies, anti-VEGF agents, and anti EGFR agentsGastric cancerLonsurf is indicated as monotherapy for the treatment of adult patients with metastatic gastric cancer including adenocarcinoma of the gastroesophageal junction, who have been previously treated with at least two prior systemic treatment regimens for advanced disease.

Tipiracil hydrochloride Use and Manufacturing

Use Classification：

Human drugs -> Lonsurf -> EMA Drug Category|Antineoplastic agents -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:279.12
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:278.0337310
Monoisotopic Mass:278.0337310
Topological Polar Surface Area:85.3
Heavy Atom Count:17
Complexity:404
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Thymidine phosphorylase inhibitors increase trifluridine exposure by inhibiting the enzyme thymidine phosphorylase, which is involved in the metabolism of trifluridine.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Trifluridine Tipipiridine Tablets
Ingredients	This product is a compound preparation, the main ingredients are trifluridine and tipiracil hydrochloride. Chemical name of trifluridine: 2'-deoxy-5-(trifluoromethyl)uridine Molecular formula: C10H11F3N2O5 Molecular weight: 296.20 Chemical name of tipiracil hydrochloride: 5-chloro-6-[(2-iminopyrrolidin-1-ylmethyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione hydrochloride Molecular formula: C9H11ClN4O2・HCl Molecular weight: 279.12 Excipients: lactose, low-substituted hydroxypropyl cellulose, magnesium stearate, film coating premix (gastric soluble).
Indication	Trifluridine is a substrate for thymidine phosphorylase and is not metabolized by cytochrome P450 (CYP) enzymes. Tipipiracil is not metabolized in human liver or hepatocytes. In vitro studies have shown that trifluridine, tipipiracil, and FTY do not inhibit CYP enzymes and have no induction effect on CYP1A2, CYP2B6, or CYP3A4/5. In vitro studies have shown that trifluridine is not an inhibitor or substrate of human uptake and efflux transporters.
Specifications	20mg x 10 tablets x 2 bags
Manufacturer	Qilu Pharmaceutical Co., Ltd.

Registered Holders

BIOPHORE INDIA PHARMACEUTICALS PVT LTD

United States
Active
MSN LABORATORIES PRIVATE LTD

United States
Active
HETERO LABS LTD

United States
Active

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Tipiracil

CAS No.: 183204-72-0

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CAS No.: 183204-72-0

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