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Vyloy

zolbetuximab
CLDN18.2-Targeting Monoclonal Antibody FDA Approved 2024 Astellas Pharma
Route
IV Infusion
Half-Life
~12 days
FDA Approved
2024
Manufacturer
Astellas Pharma
1. Indications and Usage

In combination with fluoropyrimidine- and platinum-containing chemotherapy for the first-line treatment of adults with locally advanced unresectable or metastatic HER2-negative gastric or gastroesophageal junction (GEJ) adenocarcinoma whose tumors are Claudin-18 protein 2 (CLDN18.2) positive, as determined by an FDA-approved test.

2. Dosage and Administration

Cycle 1: 800 mg/m² IV over 3 hours. Subsequent cycles: 600 mg/m² IV over 2 hours, every 3 weeks. Administer pre-medications (corticosteroid, antihistamine, antipyretic) before each dose. Administer zolbetuximab before chemotherapy on Day 1.

3. Dosage Forms and Strengths

Concentrate for solution for infusion: 100 mg/10 mL (10 mg/mL) vial

4. Contraindications

None established in prescribing information.

5. Warnings and Precautions
  • Nausea and Vomiting: Severe nausea (21% grade ≥3) and vomiting (15% grade ≥3) are common. Pre-medicate with antiemetics and continue around each infusion cycle.
  • Decreased Appetite: Common and can be severe. Monitor nutritional status.
  • Infusion-Related Reactions: IRR reported; pre-medicate and monitor during infusion.
  • Embryo-Fetal Toxicity: Can cause fetal harm. Advise effective contraception.
6. Adverse Reactions
Most Common Adverse Reactions

Nausea (83%), Vomiting (67%), Decreased appetite (46%), Fatigue (30%), Neutropenia (31%), Diarrhea (16%), Constipation (17%), Peripheral neuropathy (11%)

Nausea
83%
Vomiting
67%
Decreased appetite
46%
Fatigue
30%
Neutropenia
31%
Diarrhea
16%
Constipation
17%
Peripheral neuropathy
11%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

7. Drug Interactions

No formal drug interaction studies conducted. As a monoclonal antibody, significant PK drug-drug interactions are not anticipated.

8. Use in Specific Populations
Pregnancy

Can cause fetal harm. Advise females of reproductive potential to use effective contraception. Consult the full prescribing information for pregnancy risk details.

Lactation

Advise women not to breastfeed during treatment and for a period after the last dose. Refer to prescribing information for duration guidance.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established unless otherwise noted in the full prescribing information.

Hepatic/Renal Impairment

Dose modifications for organ impairment are specified in the complete prescribing information.

12. Clinical Pharmacology
Mechanism of Action

Zolbetuximab is a chimeric IgG1 monoclonal antibody that binds to Claudin-18 isoform 2 (CLDN18.2), a tight junction protein overexpressed in gastric and GEJ adenocarcinomas. Binding leads to antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), resulting in tumor cell lysis. CLDN18.2 is accessible on tumor cells due to disrupted tight junctions.

Pharmacokinetics

Route: IV. Vd: ~3.5 L. Protein binding: minimal (monoclonal antibody). Metabolized by proteolytic catabolism. Half-life: ~12 days. Elimination: protein catabolism pathways.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
FDA-Approved Tumor Types

Vyloy has FDA-approved indications across the following cancer types covered on CancerDrugEvidence:

External Resources
Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Vyloy. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.

Frequently Asked Questions

What is Vyloy (zolbetuximab) approved for?

Vyloy (zolbetuximab) is an FDA-approved oncology agent. Refer to the full prescribing information for complete indication details.

How is Vyloy (zolbetuximab) administered?

Refer to the full prescribing information for dosing schedules, administration instructions, and dose modifications.

How does Vyloy (zolbetuximab) work?

Zolbetuximab is a chimeric IgG1 monoclonal antibody that binds to Claudin-18 isoform 2 (CLDN18.2), a tight junction protein overexpressed in gastric and GEJ adenocarcinomas. Binding leads to antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), resulting in tum

What are the most common side effects?

Nausea (83%), Vomiting (67%), Decreased appetite (46%), Fatigue (30%), Neutropenia (31%), Diarrhea (16%), Constipation (17%), Peripheral neuropathy (11%)