Lucisel Selpercatinib 40mg 120 Capsules

Description

What is Lucisel Selpercatinib 40mg?

Selpercatinib is an effective RET kinase inhibitor, with IC50 values ​​ranging from 0.92 to 67.8 nM depending on the RET gene variant. Based on information from naturally occurring drug resistance mutations and molecular modeling studies, selpercatinib competes with ATP for binding, thereby preventing autophosphorylation of RET. Single amino acid mutations at position 810 may affect selpercatinib binding without changing ATP binding, which may cause treatment failure.

Besides, selpercatinib also showed the ability to inhibit other receptor tyrosine kinases such as VEGFR1, VEGFR3, FGFR1, FGFR2 and FGFR3, however, this effect has not been well explored in the clinical setting.

The drug Lucisel, containing the active ingredient selpercatinib, is prepared in capsule form:

– Active ingredient: Selpercatinib 40mg.

– Packaging: Box of 120 tablets.

– Origin: Lucius Laos.

Uses of Lucisel Selpercatinib 40mg

Lucisel Selpercatinib 40mg, as monotherapy, is used to treat adult subjects with the following conditions:

• Non-small cell lung cancer (NSCLC) positive for RET mutations, in cases where disease has progressed without prior treatment with a RET inhibitor.
• RET mutation-positive thyroid cancer has progressed and requires systemic treatment after having undergone treatment with sorafenib and/or lenvatinib.
• Lucisel is also indicated for adults and adolescents 12 years of age and older with advanced RET-mutant medullary thyroid cancer (MTC).

Dosage and usage of Lucisel Selpercatinib 40mg

LuciSel therapy should be initiated and monitored by physicians experienced in cancer treatment.

RET gene testing

Before initiating treatment with LuciSel, confirm the presence of a RET gene fusion in patients with non-small cell lung cancer (NSCLC) and nonmedullary thyroid cancer, or a RET mutation in patients with mutated medullary thyroid cancer (MTC) through a validated test.

Dosage of LuciSel

The recommended dosage of LuciSel depends on the patient’s body weight as follows:

– Under 50 kg: 120 mg, twice daily.

– Over 50 kg: 160 mg, twice daily.

If the patient misses a dose or vomits, they should continue taking the next dose at the scheduled time without making up for the missed dose.

Treatment should continue until disease progression or unacceptable side effects occur.

When LuciSel is coadministered with strong CYP3A inhibitors, the dose of selpercatinib should be reduced by 50%. When discontinuing a CYP3A inhibitor, the dose of selpercatinib should be adjusted back to baseline after 3 to 5 half-lives of the inhibitor.

Instructions for use

LuciSel is taken by mouth. Capsules should be swallowed whole and should not be opened, crushed or chewed before swallowing. Patients can take the medicine with or without meals. However, if taken with proton pump inhibitors, LuciSel should be taken with meals.

Additionally, the medication should be taken 2 hours before or 10 hours after taking an H2 receptor antagonist. Patients need to take the medication at approximately the same time each day to ensure optimal treatment effectiveness.

Be careful when using Luciel Selpercatinib 40mg

Interstitial Lung Disease (ILD)/Pneumonia

Cases of severe ILD/pneumonitis, even life-threatening or fatal, have been reported in patients receiving selpercatinib. Lung-related symptoms, such as difficulty breathing, cough and fever, should be closely monitored, as these may be signs of ILD. When acute or severe respiratory symptoms occur, treatment with selpercatinib should be discontinued immediately and the patient should be thoroughly investigated. Based on severity, interruption, dose reduction, or permanent discontinuation of the medication may be necessary.

Increased Liver Enzymes (ALT/AST)

Cases of increased liver enzyme levels ALT and AST grade ≥ 3 have also been reported. ALT and AST should be checked before starting treatment, then every 2 weeks for the first 3 months, and monthly for the next 3 months. Depending on the degree of liver enzyme elevation, selpercatinib dosage may need to be adjusted.

Hypertension

Increased blood pressure has been observed in patients receiving selpercatinib. Blood pressure should be controlled before and during treatment, and high blood pressure treated when necessary. If hypertension cannot be controlled with conventional therapy, selpercatinib use should be permanently discontinued.

QT Interval Prolongation

QT prolongation is another phenomenon that has been reported. Use selpercatinib with caution in patients with a history or high risk of arrhythmias. Before initiating treatment, patients should have a QTcF interval ≤ 470 ms and serum electrolytes within the normal range. ECG and serum electrolyte levels should be monitored regularly, especially after 1 week of treatment and monthly for the first 6 months.

Hypothyroidism

Hypothyroidism has also been reported in patients receiving selpercatinib. Thyroid function should be checked before and periodically throughout treatment. Patients with hypothyroidism should be treated according to standard medical guidelines. In case of necessity, patients may need liothyronine supplementation in addition to levothyroxine due to the effect of selpercatinib on thyroid hormone metabolism.

Interaction of Lucisel Selpercatinib 40mg with other drugs

When you start treatment with Selpercatinib, it is important to tell your healthcare provider about any medications you are using. This includes prescription medications, over-the-counter medications, vitamins and herbal supplements. Drug interactions may affect the effectiveness of Selpercatinib, so this information is extremely important.

You should avoid using certain medications during treatment with LuciSel to avoid harmful drug interactions, including:

– St. John’s Wort

– Proton pump inhibitors (PPIs)

– H2 blockers

– Antacids containing aluminum, magnesium, calcium, simethicone or buffering drugs