Exkivity (Mobocertinib) – NSCLC | HongKong DengYue Medicine

Exkivity Application Scope

Exkivity is an oral, first-in-class tyrosine kinase inhibitor targeting EGFR exon 20 insertion mutations in non–small cell lung cancer (NSCLC).

Characteristics

• Ingredients: Mobocertinib (fermented succinate salt)

• Properties:

  • Covalent, irreversible inhibitor of EGFR with exon 20 insertion mutations

  • Selectively binds to cysteine 797 in the EGFR active site

• Packaging Specification: Hard capsules, 40 mg each, supplied in bottles

• Storage: Store at 20 °C–25 °C (68 °F–77 °F); excursions permitted between 15 °C–30 °C

• Expiry Date: 24 months from the manufacture date when stored properly

• Executive Standard:

  • Meets FDA labeling

  • USP controlled room temperature standards

• Approval Number: FDA at NDA 215310, approved September 15, 2021

• Date of Revision: Last revised: September 2023

• Manufacturer: Takeda Pharmaceuticals International AG

Guidelines for the Use of Exkivity

• Dosage and Administration:

  • 160 mg (4 capsules of 40 mg) taken orally once daily, with or without food

  • Until disease progression or unacceptable toxicity

  • Swallow capsules whole; do not open or crush

  • Baseline and periodic monitoring of ECG, QTc, and electrolytes (Na, K, Mg, Ca)

  • Withhold or adjust dose for toxicity such as QTc prolongation,

  • Interstitial lung disease/pneumonitis, diarrhea, or cardiac toxicity

• Adverse Reactions:

  • Prevalent (>20%):

    • diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite

    • paronychia, fatigue, dry skin, musculoskeletal pain

  • Common Grade 3–4 lab abnormalities (≥2%):

    • lymphopenia, elevated amylase/lipase, decreased potassium

    • hemoglobin, magnesium; increased creatinine

• Contraindications: None listed in FDA labeling

• Precautions:

  • QTc prolongation and Torsades de Pointes:

    • boxed warning

    • avoid concomitant QT-prolonging 

    • CYP3A inhibitors/inducers; monitor closely

  • ILD/pneumonitis:

    • Monitor for respiratory symptoms

    • Withhold or discontinue if confirmed

  • Cardiac toxicity: Monitor cardiac function; withhold/resume as needed

  • Embryo-fetal toxicity:

    • May cause fetal harm;

    • Use effective non-hormonal contraception in both sexes during treatment

    • And for recommended post-treatment durations

Exkivity Interactions

• Drug Interactions:

  • CYP3A inhibitors/inducers:

    • Avoid strong/moderate inhibitors or inducers

    • Adjust the dose or avoid

  • Avoid hormonal contraceptives due to reduced effectiveness

  • Monitor QTc when combined with other QT-prolonging agents

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
• It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.