Tipanat

On November 18, 2021, Natco Pharma launched the fixed-dose combination Tipanat (Trifluridine + Tipiracil, Trifluridine + Tipiracil) in a bottle of 20 tablets under the Tipanat brand for the first time in India. Tipanat is a novel anti-tumor nucleoside analog indicated for the treatment of advanced colorectal and gastric cancer.

Approximately 1,25,000 new cases of the above cancers are reported every year in India. Tipanat will be important not only in extending survival but also in preserving quality of life in late-stage treatment, which is an unmet medical need.

Tipanat (trifluridine, tipiracil) is an oral compound nucleoside chemotherapy drug composed of trifluridine (FTD) and tipiracil (TPI) in a molar ratio of 1:0.5. Original product: LONSURF (Trifluridine/Tipiracil, FTD/TPI), produced by Japan's Dapeng Pharmaceutical.

[Mechanism of action]

LONSURF is composed of a thymidine-based nucleoside analog, trifluridine and a thymidine phosphorylase inhibitor, tipiracil, with a molar ratio of 1:0.5 (weight ratio, 1:0.471). Containing ofpipiilil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. After uptake into cancer cells, trifluridine is incorporated into DNA, interfering with DNA synthesis and inhibiting cell proliferation. Trifluridine/tipiracil exhibits antitumor activity against KRAS wild-type and mutant human colorectal cancer xenografts in mice.

[Indications and Usage]

LONSURF is a combination of trifluridine (a nucleoside metabolism inhibitor) and tipiracil (a thymidine phosphate Acidase inhibitor) combination for the treatment of adult patients with: 1) metastatic colorectal cancer who have previously received fluoropyrimidine, oxaliplatin, and irinotecan-based chemotherapy, anti-VEGF biologic therapy, and RAS wild-type, anti-EGFR therapy. 2) Metastatic gastric or gastroesophageal junction adenocarcinoma, treated with at least two chemotherapy regimens, including fluoropyrimidine, platinum, taxane or irinotecan, and HER2/neu targeted therapy.

[Dosage and Administration]

Recommended dose: 35 mg/m2/dose orally twice a day, taken from the 1st to the 5th and the 8th to the 12th day of 28 days a day.

[Dosage form and strength]

Tablet: 15mg trifluridine/6.14mg tipiracil • 20mg trifluridine/8.19mg tipiracil There are no contraindications.

[Warnings and Precautions]

Severe Myelosuppression: Obtain a complete blood count before and after Day 15 of each cycle. Withhold and resume the next lower LONSURFdosage as recommended.

Embryo-Fetotoxicity: May cause fetal harm. Inform women of their reproductive potential and of the potential risks to the fetus and to use effective infections.

[Adverse Reactions]

The most common adverse reactions or laboratory abnormalities (≥10%) are regional anemia, neutropenia, fatigue/weakness, nausea, thrombocytopenia, atrophy, diarrhea, vomiting and pyrexia.

[For specific groups of people]

Lactating period: It is recommended not to breastfeed.

Geriatric Use: Neutropenia and thrombocytopenia at 3 or 4 years of age and grade 3 anemia are more common in patients 65 years of age or older.

Hepatic Impairment: Do not initiate LONSURF in patients with moderate or severe baseline hepatic impairment.