Selcaxen is a potent kinase inhibitor containing Selpercatinib, designed for the targeted treatment of cancers driven by RET (rearranged during transfection) alterations. It is effective in patients with medullary thyroid cancer (MTC), RET fusion-positive thyroid cancer, and other RET-driven malignancies. Selcaxen selectively inhibits wild-type RET and multiple RET mutations, as well as VEGFR1 and VEGFR3, preventing tumor cell proliferation and promoting anti-tumor activity.

Selcaxen’s oral formulation allows convenient administration, and it is suitable for adult and pediatric patients (≥12 years) requiring systemic therapy. By specifically targeting oncogenic RET signaling, Selcaxen offers precise tumor control while minimizing effects on non-cancerous cells.

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Therapeutic Class

Cytotoxic chemotherapy / Kinase inhibitor

Pharmacology

• Mechanism of Action: Selpercatinib inhibits RET kinase activity, blocking downstream signaling pathways essential for tumor growth.

• Selectivity: Demonstrates high potency against RET and RET-mutated isoforms, with lower activity against VEGFRs and FGFRs at clinically relevant concentrations.

• Effect on Tumor Cells: Reduces proliferation and induces tumor cell death in RET-driven cancers.

Indications

Selcaxen is indicated for:

• RET fusion-positive thyroid cancer refractory to radioactive iodine therapy

• Medullary thyroid cancer (MTC) requiring systemic therapy

• RET-driven advanced or metastatic solid tumors in eligible patients

Dosage and Administration

• Recommended Dose: Take Selcaxen orally twice daily (approximately every 12 hours) until disease progression or unacceptable toxicity

• Swallow capsules whole; do not crush or chew

• In case of missed dose, take only if >6 hours remain until the next dose

• Special instructions: Avoid concomitant use with PPIs, H2 blockers, or antacids; if unavoidable, adjust timing or take with food

Dose modifications may be required in patients with severe hepatic impairment or when co-administered with strong CYP3A inhibitors.

Drug Interactions

• Acid-reducing agents: Can reduce plasma concentrations and anti-tumor activity

• CYP3A inhibitors: Increase Selcaxen plasma levels; monitor for QT prolongation

• CYP3A inducers: Decrease Selcaxen levels; avoid use

• Enzyme and transporter effects: May affect substrates of CYP3A4, P-gp, BCRP, and OATP1B1; monitor or adjust concomitant medications

Side Effects

Most common side effect:

• Constipation

Other serious but less common effects include:

• Hepatic adverse reactions

• Hypertension

• QT interval prolongation

• Hemorrhagic events

• Hypersensitivity reactions

• Tumor lysis syndrome

Patients should be monitored regularly for blood pressure, liver function, QT interval, and signs of hemorrhage.

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Pregnancy and Lactation

• Can cause fetal harm; advise against pregnancy during treatment

• Breastfeeding should be avoided during treatment and for 1 week after the last dose

Precautions & Warnings

• Monitor hepatic function (ALT/AST) and blood pressure

• Use caution in patients with cardiac disease or QT prolongation risk

• Monitor for hypersensitivity reactions and tumor lysis syndrome

• Pediatric use: Safety established for ≥12 years; monitor growth plates in adolescents

• No dosage modification required for mild-to-moderate renal impairment; adjust for severe hepatic impairment

Storage Conditions

Store below 30°C in a cool, dry place, protected from light. Keep out of reach of children.