Alectinib

Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations.

• ALECENSA is a kinase inhibitor indicated for: adjuvant treatment in adult patients following tumor resection of anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) (tumors ≥ 4 cm or node positive) as detected by an FDA-approved test. ( 1.1 ) treatment of adult patients with ALK-positive metastatic NSCLC as detected by an FDA-approved test.ICD-10: C34.90, C85.90

• None. None.contraindicated

600 mg orally twice daily. Administer ALECENSA with food. ( 2.2 ) 2.1 Patient Selection Select patients with resectable tumors for the adjuvant treatment of NSCLC with ALECENSA based on the presence of ALK positivity in tumor tissue [see Indications and Usage (1.1) and Clinical Studies (14.1) ]. Select patients for the treatment of metastatic NSCLC with ALECENSA based on the presence of ALK positivity in tumor tissue or plasma specimens [see Indications and Usage (1.2) and Clinical Studies (14.2) ] . If ALK rearrangements are not detected in a plasma specimen, test tumor tissue if feasible. Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics. 2.2 Dosing and Administration The recommended dosage information for ALECENSA is provided in Table 1 . Table 1: ALECENSA Recommended Dosage and Duration of Treatment Indication Recommended Dosage of ALECENSA Duration Adjuvant treatment of resected NSCLC 600 mg orally twice daily with food [see Clinical Pharmacology (12.3) ] For a total of 2 years or until disease recurrence or unacceptable toxicity Metastatic NSCLC Until disease progression or unacceptable toxicity Swallow capsules whole, do not open or dissolve the contents of the capsule. If a dose of ALECENSA is missed or vomiting occurs after taking a dose of ALECENSA, take the next dose at the scheduled time.

Hepatotoxicity: Monitor liver laboratory tests every 2 weeks during the first 3 months of treatment, then once a month and as clinically indicated, with more frequent testing in patients who develop transaminase and bilirubin elevations. In case of severe ALT, AST, or bilirubin elevations, withhold, then reduce dose, or permanently discontinue ALECENSA. ( 2.4 , 5.1 ) Interstitial Lung Disease (ILD)/Pneumonitis: Immediately withhold ALECENSA in patients diagnosed with ILD/pneumonitis and permanently discontinue if no other potential causes of ILD/pneumonitis have been identified. ( 2.4 , 5.2 ) Renal Impairment: Withhold ALECENSA for severe renal impairment, then resume ALECENSA at reduced dose upon recovery or permanently discontinue ( 2.4 , 5.3 ). Bradycardia: Monitor heart rate and blood pressure regularly. If symptomatic, withhold ALECENSA then reduce dose, or permanently discontinue. ( 2.4 , 5.4 ) Severe Myalgia and Creatine Phosphokinase (CPK) Elevation: Assess CPK every 2 weeks during the first month of treatment and in patients reporting unexplained muscle pain, tenderness, or weakness. In case of severe CPK elevations, withhold, then resume or reduce dose. ( 2.4 , 5.5 ) Hemolytic Anemia: If hemolytic anemia is suspected, withhold ALECENSA. If hemolytic anemia is confirmed, consider resuming at a reduced dose upon resolution or permanently discontinue. ( 5.6 ) Embryo-Fetal Toxicity: ALECENSA can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.

The following adverse reactions are discussed in greater detail in other sections of the label: Hepatotoxicity [see Warnings and Precautions (5.1) ] Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.2) ] Renal Impairment [see Warnings and Precautions (5.3) ] Bradycardia [see Warnings and Precautions (5.4) ] Severe Myalgia and Creatine Phosphokinase (CPK) Elevation [see Warnings and Precautions (5.5) ] Hemolytic Anemia [see Warnings and Precautions (5.6) ] Embryo-Fetal Toxicity [see Warnings and Precautions (5.7) ] The most common adverse reactions (incidence ≥20%) were hepatotoxicity, constipation, fatigue, myalgia, edema, rash and cough. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Genentech at 1-888-835-2555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled safety population described in the WARNINGS AND PRECAUTIONS reflect exposure to ALECENSA as a single agent at 600 mg orally twice daily in 533 patients in Studies NP28761, NP28673, ALEX and ALINA [see Clinical Studies (14) ]. Among 533 patients who received ALECENSA, 75% were exposed for 6 months or longer and 64% were exposed for greater than one year.

Lactation: Do not breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, ALECENSA can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available data on ALECENSA use in pregnant women. Administration of alectinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in embryo-fetal toxicity and abortion at maternally toxic doses with exposures approximately 2.7-fold those observed in humans treated with alectinib at 600 mg twice daily (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In a preliminary rabbit embryo-fetal study, administration of alectinib by oral gavage during the period of organogenesis resulted in abortion or complete embryo-fetal mortality at a maternally toxic dose of 27 mg/kg/day (approximately 2.9-fold the estimated area under the curve (AUC 0-24h,ss ) in humans treated with alectinib 600 mg twice daily) in three of six pregnant rabbits. The remaining three pregnant rabbits in this group had few live fetuses, decreased fetal and placental weights, and retroesophageal subclavian artery.

Metabolism

The pharmacokinetics of alectinib and its major active metabolite M4 have been characterized in patients with ALK-positive NSCLC and healthy subjects. In patients with ALK-positive NSCLC, the geometric mean (coefficient of variation %) steady-state maximal concentration (C max,ss ) for alectinib was 665 ng/mL (44%) and for M4 was 246 ng/mL (45%) with peak to trough concentration ratio of 1.2.

No experience with overdose is available. There is no specific antidote for overdose with ALECENSA. Alectinib and its major active metabolite M4 are > 99% bound to plasma proteins; therefore, hemodialysis is likely to be ineffective in the treatment of overdose.

• Dec 11, 2015NDANDA208434Hoffmann-la Roche

1. 1Death6879.7%
2. 2Fatigue5067.1%
3. 3No Adverse Event4646.5%
4. 4Off Label Use4556.4%
5. 5Constipation4376.2%
6. 6Rash2563.6%
7. 7Dyspnoea2313.3%
8. 8Myalgia2072.9%
9. 9Weight Increased2062.9%
10. 10Disease Progression2012.8%
11. 11Asthenia1872.6%
12. 12Peripheral Swelling1752.5%
13. 13Drug Ineffective1682.4%
14. 14Pain1602.3%
15. 15Nausea1572.2%

The 10 most recently updated of 95 ClinicalTrials.gov registrations naming Alectinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Rollover Study of Alectinib in Patients With Anaplastic Lymphoma Kinase (ALK)-Positive or Rearranged During Transfection (RET)-Positive Cancer
  Completed · Phase 3 · Interventional · 50 enrolled · Hoffmann-La Roche
  NCT03194893updated 2026-06-11
• A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC)
  Recruiting · Phase 2 · Interventional · 99 enrolled · Genentech, Inc.
  NCT04302025updated 2026-06-09
• A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC)
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 1,000 enrolled · Hoffmann-La Roche
  NCT03178552updated 2026-06-05
• A Study Evaluating the Safety, Pharmacokinetics, and Efficacy of Alectinib in Pediatric Participants With ALK Fusion-Positive Solid or CNS Tumors
  Recruiting · Phase 1 · Phase 2 · Interventional · 42 enrolled · Hoffmann-La Roche
  NCT04774718updated 2026-06-04
• Real World Clinical Outcomes of Resected ALK-Positive Early Stage NSCLC Patients Treated With Alectinib as Adjuvant Therapy
  Recruiting · Observational · 800 enrolled · Hoffmann-La Roche
  NCT06862869updated 2026-06-04
• Neladalkib (NVL-655) for TKI-naive Patients With Advanced ALK-Positive NSCLC
  Recruiting · Phase 3 · Interventional · 450 enrolled · Nuvalent Inc.
  NCT06765109updated 2026-06-02
• Pharmacogenomics IND EXEMPT SNP Clinical Trial - Alectinib and Single Nucleotide Polymorphisms
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 600 enrolled · Han Xu, M.D., Ph.D., FAPCR, Sponsor-Investigator, IRB Chair
  NCT05987956updated 2026-06-01
• A Study Comparing Alectinib With Crizotinib in Treatment-Naive Anaplastic Lymphoma Kinase-Positive Advanced Non-Small Cell Lung Cancer Participants
  Completed · Phase 3 · Interventional · 303 enrolled · Hoffmann-La Roche
  NCT02075840updated 2026-05-29
• A Study of Neladalkib (NVL-655) in Patients With Advanced NSCLC and Other Solid Tumors Harboring ALK Rearrangement or Activating ALK Mutation (ALKOVE-1)
  Recruiting · Phase 1 · Phase 2 · Interventional · 840 enrolled · Nuvalent Inc.
  NCT05384626updated 2026-05-27
• A Study of Alectinib and Duvelisib in People With Anaplastic Lymphoma Kinase-Positive Anaplastic Large Cell Lymphoma (ALK+ALCL)
  Recruiting · Phase 1 · Interventional · 30 enrolled · Memorial Sloan Kettering Cancer Center
  NCT07001384updated 2026-05-26

Frequently asked questions

How does Alectinib work?

Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations.

What is Alectinib used for?

According to FDA labeling, Alectinib carries indications including: ALECENSA is a kinase inhibitor indicated for: adjuvant treatment in adult patients following tumor resection of anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) (tumors ≥ 4 cm or node positive) as detected by an FDA-approved test. ( 1.1 ) treatment of adult patients with ALK-positive metastatic NSCLC as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Alectinib?

Alectinib is classified as Anaplastic lymphoma kinase (ALK) inhibitors, Kinase Inhibitor, Kinase Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Alectinib?

Alectinib is marketed under brand names including Alecensa.

What are the contraindications for Alectinib?

Alectinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.