1 / 2

Selumetinib(Koselugo)

Acetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine Injection

Reference price:

Manufacturer:

Formulation:

CAPSULE

Validity period:

Not specified in the specification.

Reminder: The outer packaging is for reference only, please purchase and use under the guidance of a pharmacist. For read by medical and pharmaceutical professionals only.

KOSELUGO (selumetinib) is an orally administered, selective inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), which are key components of the RAS-RAF-MEK-ERK signaling pathway. This pathway is frequently dysregulated in various cancers and genetic disorders, including NF1. By inhibiting MEK1/2, selumetinib disrupts downstream signaling involved in cell proliferation and survival, thereby reducing tumor growth and associated morbidity in affected patients.

Clinically, KOSELUGO has demonstrated efficacy in reducing the volume of inoperable plexiform neurofibromas in pediatric patients with NF1, as evidenced by response rates in pivotal clinical trials. The drug is available in capsule form (10 mg and 25 mg strengths) and is administered based on body surface area, with dosing adjustments required for hepatic impairment and certain drug interactions. KOSELUGO represents a targeted therapeutic option for a population with limited alternative treatments.

Generic name

Selumetinib(Koselugo)

English name

Selumetinib

Alternative Names

Koselugo

Drug prices

Indications

KOSELUGO is indicated for the treatment of pediatric patients aged 2 years and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN).

Therapeutic Target

KOSELUGO targets mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), which are key components of the RAS-RAF-MEK-ERK signaling pathway.

Active Ingredients

Selumetinib (as selumetinib sulfate).

Dosage form

CAPSULE

specifications

Supplied in bottles of 28 or 60 capsules.

Description

Selumetinib is a selective MEK1/2 inhibitor. The chemical name is 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-6-[(2-hydroxyethoxy)carbamoyl]-1-methyl-1H-benzimidazol-3-ium hydrogen sulfate. It is a white to yellow monomorphic crystalline powder, freely soluble at pH <1.5, sparingly soluble at pH 1.5–3, and slightly soluble at pH >3. Each 10 mg capsule contains 32 mg vitamin E as D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS); each 25 mg capsule contains 36 mg vitamin E as TPGS.

Dosage and Administration

Recommended dose: 25 mg/m² orally twice daily (approximately every 12 hours), with or without food, until disease progression or unacceptable toxicity.

Dose is based on body surface area (BSA), with specific dosing bands provided.

Dose reductions are required for moderate hepatic impairment (Child-Pugh B) and for certain drug interactions (e.g., CYP3A4 inhibitors).

Capsules must be swallowed whole with water; do not chew, dissolve, or open.

Missed doses should not be taken unless more than 6 hours remain until the next scheduled dose.

If vomiting occurs after administration, do not take an additional dose; continue with the next scheduled dose.

CATEGORY NAVIGATION