Tucatinib/Tucatinib detailed instructions

1. Indications and Usage

Tucatinib/Tucatinibis a kinase inhibitor:

In combination with trastuzumab and capecitabine, it is indicated for the treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

In combination with trastuzumab, it is indicated for the treatment of adult patients with RASwild-typeHER2-positive unresectable or metastatic colorectal cancer that has progressed after treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy.

This indication received accelerated approval based on tumor response rate and durability of response. Continued approval for this indication may be contingent on verification and characterization of clinical benefit in confirmatory trials.

2. Dosage and usage

Before starting tucatinib, confirm the presence of HER2protein overexpression and RASwild type in tumor specimens.

Recommended dose: 300 mg orally, twice daily, with or without food.

For patients with severe hepatic impairment, the recommended dose is 200 mg orally twice daily.

Three. Dosage form and strength

Tablets: 50mg and 150mg.

Four. Contraindications

No.

Five. Warnings and Precautions

1.Diarrhea. Tucatinibcan cause severe diarrhea, including dehydration, hypotension, acute kidney injury, and death. If diarrhea occurs, treat with antidiarrheal medications as clinically indicated. Diagnostic testing is performed as clinically indicated to rule out other causes of diarrhea. Depending on the severity of diarrhea, interrupt dose, then reduce dose or permanently discontinue tucatinib.

2.Hepatotoxicity

Tucatinibcan cause severe hepatotoxicity. Monitor ALT, AST and bilirubin before initiatingtucatinib, every 3 weeks during treatment, and as clinically indicated. Depending on the severity of hepatotoxicity, interrupt dose and then reduce dose or permanently discontinue tucatinib.

3.Embryo-Fetal Toxicity. Based on the results of animal studies and its mechanism of action, taking tucatinib by pregnant women may cause harm to the fetus. In animal reproduction studies, administration of tucatinib to pregnant rats and rabbits during organogenesis resulted in fetal death, reduced fetal weight, and fetal malformations (maternal exposure ≥ 1.3 times the recommended human exposure (AUC)). Inform pregnant women and women of reproductive potential of the potential risk to the fetus and advise women of childbearing potential to use effective contraception during treatment with tucatinib and for 1 weeks after the last dose. Advise male patients with a female partner of childbearing potential to use effective contraception during treatment with tucatinib and for 1 week after the last dose.

6. Adverse reactions

The most common adverse reactions (≥20%) of tucatinib in combination with trastuzumab and capecitabine in patients with metastatic breast cancer are diarrhea, palmoplantar red blood cell paresthesia, nausea, hepatotoxicity, vomiting, stomatitis, decreased appetite, anemia, and rash.

The most common adverse reactions (≥20%) in patients with unresectable or metastatic colorectal cancer treated with tucatinib combined with trastuzumab are diarrhea, fatigue, rash, nausea, abdominal pain, infusion-related reactions and fever.

7. Drug interactions

StrongCYP3AInducers or moderateCYP2C8Inducers:Avoid concurrent use.

StrongCYP2C8 inhibitor:Avoid concomitant use; if concomitant use cannot be avoided, reduce tucatinib dose.

CYP3ASubstrates:Avoid concurrent use with CYP3A substrates as minimal concentration changes may result in serious or life-threatening toxicity.

P-gpSubstrates:Consider reducing the dosage ofP-gpsubstrates where minimal concentration changes may result in serious or life-threatening toxicity.

8. Use among specific groups of people

Breastfeeding:Breastfeeding is not recommended. There is a generic version of this drug in Bangladesh. The retail price of Everest Pharmaceuticals in Bangladesh is about 150mg30 tablets6000 yuan. The retail price of Ziska Pharmaceuticals in Bangladesh is around 4,500 yuan for 150 mg 30 tablets. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to help you learn more about high-quality overseas drugs.

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