Trifluridine and tipiracil

What is Trifluridine and tipiracil?[edit | edit source]

It is a nucleoside metabolic inhibitor
It is a white crystalline powder, soluble in water, ethanol, 0.01 mol/L hydrochloric acid, 0.01 mol/L sodium hydroxide solution; freely soluble in methanol, acetone; sparingly soluble in 2-propanol, acetonitrile; slightly soluble in diethyl ether; and very slightly soluble in isopropyl ether.
Chemical name: 2’-deoxy-5-(trifluoromethyl) uridine
Molecular formula: C10H11F3N2O5
Molecular weight: 296.20

It is a thymidine phosphorylase inhibitor
Tipiracil hydrochloride is a white crystalline powder, soluble in water, 0.01 mol/L hydrochloric acid, and 0.01 mol/L sodium hydroxide; slightly soluble in methanol; very slightly soluble in ethanol; and practically insoluble in acetonitrile, 2-propanol, acetone, diisopropyl ether, and diethyl ether.
Chemical name: 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4-(1H,3H)-dione monohydrochloride or 2,4(1H,3H)-Pyrimidinedione, 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-, hydrochloride (1:1)
Molecular formula: C9H11ClN4O2•HCl
Molecular weight: 279.12

It is indicated for the treatment of adult patients with metastatic colorectal cancer previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.
It is indicated for the treatment of adult patients with metastatic gastric or gastroesophageal junction adenocarcinoma 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.

Lonsurf consists of a thymidine-based nucleoside analog, trifluridine, and the thymidine phosphorylase inhibitor, tipiracil, at a molar ratio 1:0.5 (weight ratio, 1:0.471).
Inclusion of tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase.
Following uptake into cancer cells, trifluridine is incorporated into DNA, interferes with DNA synthesis and inhibits cell proliferation. Trifluridine/tipiracil demonstrated anti-tumor activity against KRAS wild-type and mutant human colorectal cancer xenografts in mice.

This medicine have no usage limitations.

Brand name: Lonsurf; NDC Code(s): 64842-1020-1, 64842-1020-2, 64842-1020-3, 64842-1025-1, 64842-1025-2, 64842-1025-3.
Tablets:

15 mg trifluridine/6.14 mg tipiracil: white, biconvex, round, film-coated, imprinted with ‘15’ on one side, and ‘102’ and ‘15 mg’ on the other side, in gray ink.
20 mg trifluridine/8.19 mg tipiracil: pale red, biconvex, round, film-coated, imprinted with ‘20’ on one side, and ‘102’ and ‘20 mg’ on the other side, in gray ink.

It is approved by US FDA on Feb 25, 2019 for Adult Patients with Previously Treated Advanced Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma and on Sep 22, 2015 it is approved for advanced Colorectal Cancer.

Take Lonsurf exactly as your healthcare provider tells you.
Lonsurf comes in two strengths. Your healthcare provider may prescribe both strengths for your prescribed dose.
Take Lonsurf 2 times a day with food.
Swallow Lonsurf tablets whole.
Your caregiver should wear gloves when handling Lonsurf tablets.
If you miss a dose of Lonsurf, do not take additional doses to make up for the missed dose. Call your healthcare provider for instructions about what to do for a missed dose.
Wash your hands after handling the Lonsurf tablets.

In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

Overdose related information is also available online at poisonhelp.org/help.
In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Safety and effectiveness of Lonsurf in pediatric patients have not been established.

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F)
If stored outside of original bottle, discard after 30 days.

Trifluridine and tipiracil Resources
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