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Fakzynja

defactinib
FAK InhibitorFDA Approved 2025Verastem Oncology
Route
Oral
Half-Life
~2 hrs
FDA Approved
2025
Manufacturer
Verastem Oncology
1. Indications and Usage

In combination with avutometinib (Avmapki) for adults with KRAS-mutated previously treated low-grade serous ovarian cancer.

2. Dosage and Administration

200 mg orally twice daily in combination with avutometinib on Days 1-21 of each 28-day cycle.

3. Dosage Forms and Strengths

Tablets: 200 mg

4. Contraindications

None listed in the prescribing information.

5. Warnings and Precautions
  • Retinal Toxicity: Ophthalmologic exams at baseline and during treatment.
  • Hepatotoxicity: Monitor liver function.
  • Embryo-Fetal Toxicity: Can cause fetal harm.
6. Adverse Reactions
Most Common Adverse Reactions

Diarrhea (56%), Nausea (48%), Fatigue (42%), Rash (38%), Vomiting (32%), Edema (28%), Increased Creatinine (22%)

Diarrhea
56%
Nausea
48%
Fatigue
42%
Rash
38%
Vomiting
32%
Edema
28%
Increased Creatinine
22%

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

7. Drug Interactions

Strong CYP3A4 Inhibitors: Avoid.
Strong CYP3A4 Inducers: Avoid.

8. Use in Specific Populations
Pregnancy

Consult the full prescribing information for pregnancy-related considerations.

Lactation

Refer to prescribing information for lactation guidance.

Pediatric Use

Pediatric safety and efficacy information is detailed in the full label.

Hepatic/Renal Impairment

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

12. Clinical Pharmacology
Mechanism of Action

Defactinib is a selective oral inhibitor of focal adhesion kinase (FAK), disrupting compensatory signaling that tumors use to escape MAPK pathway blockade, synergizing with avutometinib.

Pharmacokinetics

Tmax: 1-2 hours. Protein binding: ~93%. Metabolized by CYP3A4. Half-life: ~4 hours.

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

Fakzynja 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 Fakzynja. 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 Fakzynja (defactinib) approved for?

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

How is Fakzynja (defactinib) administered?

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

How does Fakzynja (defactinib) work?

Defactinib is a selective oral inhibitor of focal adhesion kinase (FAK), disrupting compensatory signaling that tumors use to escape MAPK pathway blockade, synergizing with avutometinib.

What are the most common side effects?

Diarrhea (56%), Nausea (48%), Fatigue (42%), Rash (38%), Vomiting (32%), Edema (28%), Increased Creatinine (22%) Diarrhea 56% Nausea 48% Fatigue 42% Rash 38% Vomiting 32% Edema 28% Increased Creatinine 22%