Dacomitinib (dacomitinib) drug instructions and precautions for use

Dacomitinib (also known as dacomitinib, English name: Dacomitinib) is a second-generation EGFRtyrosine kinase inhibitor (EGFR-TKI), developed by Pfizer, is mainly used to treat patients with non-small cell lung cancer (NSCLC) who have epidermal growth factor receptor (EGFR) sensitive mutations. Its unique irreversible binding mechanism and high affinity to multiple HER family members enable it to demonstrate superior efficacy in certain EGFR mutant lung cancers. The following is a detailed introduction to the contents of the dacomitinib package insert and precautions for use for the reference of clinicians and patients.

1. Basic drug information

Common name: Dacomitinib (Dacomitinib)

Product name: VIZIMPRO (VIZIMPRO)

Indications:

Dacomitinib is suitable for the first-line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) positive for EGFR gene-sensitive mutations (such as Exon 19 deletions or L858R mutations).

Dosage forms and specifications:

At present, the common dosage forms in China are oral tablets. The main specifications include 15mg, 30mg and 45mg. Each box is commonly packed with 30 tablets.

2. Recommended usage and dosage

Recommended dose: The standard recommended starting dose of dacomitinib is 45 mg once daily, taken orally continuously without interruption. The medicine should be swallowed whole, before or after meals.

Dosage adjustment:

If the patient experiences serious adverse reactions (such as rash, diarrhea, or abnormal liver function, etc.) during treatment, the dose may need to be adjusted according to the guidance of the doctor. The common adjusted dose is 30mg or 15mg. If it is necessary to suspend medication, the decision on whether to resume treatment and resume dosage should be based on disease assessment.

3. Pharmacological mechanism and characteristics

Dacomitinib belongs to the second generationEGFR-TKI. Compared with the first generation drugs (such as gefitinib and erlotinib), it has the following advantages:

Irreversible binding: Dacomitinib can irreversibly bind to EGFR, HER2 and HER4 and other HER family receptors, thereby continuously inhibiting signaling pathways and delaying the occurrence of drug resistance;

Covering a variety of mutations: It also has a certain inhibitory effect on some uncommonEGFR mutations;

ExtendedPFS:ARCHER 1050Clinical studies have shown that dacomitinib can significantly extend the progression-free survival (PFS) and overall survival (OS) of patients with first-line treatment of EGFRmutatedNSCLC.

4. Common adverse reactions and coping methods

Dacomitinib has relatively many adverse reactions, especially in the skin and gastrointestinal tract. The following are common side effects and treatment suggestions:

Skin rash: It is common on the face, chest and back and other parts of the body. It usually appears within 2-3 weeks after taking the medication. It is recommended to use low-intensity topical steroid ointments or oral antihistamines; in severe cases, suspension or reduction of dosage should be considered.

Diarrhea: It is one of the most common adverse reactions. It is recommended to use antidiarrheal drugs such as loperamide; electrolytes and kidney function need to be monitored in case of massive diarrhea.

Oral mucositis: Symptoms of pain or ulcers in the mouth that can be relieved with gargles or topical analgesics.

Abnormal liver function: Liver enzyme indicators should be monitored regularly, and the dosage should be reduced or suspended if necessary.

Paronychia and dry skin: Keep the skin clean and dry and avoid scratching and unnecessary irritation.

5. Pay attention to medication for special groups of people

Patients with impaired liver and renal function: Patients with mild liver and renal dysfunction usually do not need to adjust the dose, but patients with moderate to severe impairment should use it with caution, and it is recommended that the dose be individualized under the guidance of a doctor.

Elderly patients: They may be more sensitive to drugs and should strengthen monitoring of adverse reactions.

Pregnant and lactating women: There is insufficient human data to show the specific effects of dacomitinib on the fetus. Animal experiments have shown reproductive toxicity, so its use should be avoided during pregnancy. It is not clear whether dacomitinib is secreted through milk during lactation. It should be used with caution after weighing the pros and cons.

Children: There are currently no research data on the use of dacomitinib in children and its use is not recommended.

6. Drug interactions

Dacomitinib is metabolized by CYP2D6 and CYP3A4, so when using it, it should be avoided to combine with strong CYP enzyme inducers (such as rifampicin, carbamazepine) or inhibitors (such as ketoconazole) to prevent affecting the blood concentration of the drug. In addition, dacomitinib itself can also affect the metabolism of other drugs, so attention should be paid to the drug combination.

7. Monitoring recommendations during medication

Before taking medication for the first time: perform EGFR mutation testing to ensure that the patient has a sensitive mutation type;

During treatment: It is recommended to check blood routine, liver and kidney function, electrolytes and skin every2-4 weeks;

Imaging evaluation: Perform CT and other evaluations every 6-8 weeks to determine the tumor response;

Resistance monitoring: When the disease progresses, it is recommended to conduct genetic testing again to evaluate whether drug resistance mutations such as T790M have occurred so that subsequent treatment options can be changed.

Dacomitinib (dacomitinib), as a second-generation EGFR-TKI, is an important first-line targeted treatment option for patients with EGFR mutation-positive advanced non-small cell lung cancer. Its irreversible mechanism of action and broad HER family inhibitory effects bring patients longer progression-free survival. However, the drug has a high incidence of adverse reactions, especially in the skin and gastrointestinal system. Patients should closely cooperate with doctors in monitoring and management during medication to ensure that while maximizing efficacy, side effects are reduced and better quality of life and treatment effects are achieved.

Reference materials:https://www.drugs.com