Alectinib is an anaplastic lymphoma kinase (ALK) inhibitor indicated for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Indications of Alectinib 

1.1 Adjuvant treatment:

(1) For adult patients with ALK-positive NSCLC following complete tumor resection, with tumor diameter ≥4 cm or lymph node positivity.

(2) Treatment continues for 2 years or until disease recurrence.

1.2 Treatment of metastatic lung cancer:

For adult patients with ALK-positive metastatic NSCLC as confirmed by an FDA-approved test, continued until disease progression or unacceptable toxicity.

1.3 Patient selection requirements:

For adjuvant treatment, ALK positivity must be confirmed by tumor tissue testing; for metastatic treatment, confirmation may be via tumor tissue or plasma specimen. If ALK rearrangement is not detected in plasma, tumor tissue testing should be performed if possible.

Contraindications

2.1 No absolute contraindications:

According to the official prescribing information, alectinib has no absolute contraindications.

2.2 Relative precautions:

Caution or dose adjustment is required in patients with severe hepatic impairment, renal impairment, bradycardia, interstitial lung disease, etc.

Contraindicated foods and drug interactions

3.1 Drug interactions:

(1) Coadministration with strong CYP3A inhibitors (e.g., posaconazole) or strong CYP3A inducers (e.g., rifampicin) has no clinically significant effect on alectinib exposure.

(2) Coadministration with acid-reducing agents (e.g., esomeprazole) also has no significant effect.

3.2 Effects on other drugs:

Alectinib has no clinically significant effect on CYP3A substrates (midazolam) or CYP2C8 substrates (repaglinide), but may inhibit P-glycoprotein and breast cancer resistance protein.

Use in special populations – Hepatic impairment

4.1 Mild to moderate impairment:

No dose adjustment is required for patients with Child-Pugh class A or B.

4.2 Severe impairment:

For patients with Child-Pugh class C, drug exposure is increased; the recommended dose is reduced to 450 mg twice daily.

Use in special populations – Renal impairment

5.1 Mild to moderate impairment:

No dose adjustment is required for patients with creatinine clearance 30-89 mL/min.

5.2 Toxicity management:

For grade 3 renal toxicity, withhold treatment and resume at a reduced dose; for grade 4 renal toxicity, permanently discontinue.

Use in special populations – Reproductive considerations

6.1 Pregnancy:

Use during pregnancy may cause fetal harm.

6.2 Contraception requirements:

(1) Females of childbearing potential should use effective contraception during treatment and for 5 weeks after the last dose.

(2) Male patients with female partners of childbearing potential should use contraception during treatment and for 3 months after the last dose.

6.3 Lactation:

Breastfeeding is not recommended; it may be resumed at least 1 week after the last dose.

Use in special populations – Other groups

7.1 Elderly patients:

In patients aged 65 years and older, the incidence of serious adverse events, discontinuation rates, and dose adjustment rates are higher than in younger patients; enhanced monitoring is required.

7.2 Pediatric patients:

Safety and efficacy have not been established.