Trifluridine and tipiracil

What is Trifluridine and tipiracil?

Trifluridine and tipiracil

• Trifluridine:

1. It is a nucleoside metabolic inhibitor
2. 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.
3. Chemical name: 2’-deoxy-5-(trifluoromethyl) uridine
4. Molecular formula: C10H11F3N2O5
5. Molecular weight: 296.20

• Tipiracil hydrochloride:

1. It is a thymidine phosphorylase inhibitor
2. 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.
3. 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)
4. Molecular formula: C9H11ClN4O2•HCl
5. Molecular weight: 279.12

What are the uses of this medicine?

• 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.

How does this medicine work?

• 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.

Who Should Not Use this medicine?

This medicine have no usage limitations.

What are the brand names and dosage forms of this medicine?

• 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:

1. 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.
2. 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.

Is this medicine FDA approved?

• 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.

What are the active and inactive ingredients in Trifluridine and tipiracil?

• Active ingredients:

1. Trifluridine
2. Tipiracil Hydrochloride

• Inactive ingredients:

1. Lactose Monohydrate
2. Starch, Corn
3. Stearic Acid
4. Hypromellose, Unspecified
5. Polyethylene Glycol, Unspecified
6. Titanium Dioxide
7. Magnesium Stearate
8. Alcohol
9. Butyl Alcohol

How should this medicine be used?

• 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.

What side effects can this medication cause?

• Tiredness (fatigue, weakness)
• Nausea
• Decreased appetite
• Diarrhea
• Vomiting
• Abdominal pain
• Fever

What to do in case of emergency/overdose?

• 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.

Can this medicine be used in pregnancy?

• Lonsurf can cause fetal harm.
• Advise pregnant women of the potential risk to a fetus.

Can this medicine be used in children?

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

What should I know about storage and disposal of this medication?

• 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.

• Dailymed label info on Trifluridine and tipiracil
• FDA Trifluridine and tipiracil

Trifluridine and tipiracil Resources
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