​Is Selpercatinib treatment effective?

In May 2020, Selpercatinib was approved by the FDA for the treatment of various cancers caused by RET gene mutations. The drug stops the spread of the lesion by interfering with the signaling pathways of cancer cells. Clinical studies have shown that it has shown good efficacy in multiple cancer types.

Is Selpercatinib treatment effective?

Treatment-naïve patients with RET fusion-positive non-small cell lung cancer

1. Objective response rate (ORR)

63%, similar to the combination chemotherapy group, indicating significant effectiveness in treatment-naïve patients.

2. Intracranial lesion response

Of the 5 patients with CNS metastases at baseline, 4 patients experienced a treatment response to intracranial lesions, further confirming the effectiveness of this treatment for treatment-naïve patients with brain metastases.

3. Duration of intracranial remission

Among treatment-naïve patients who responded to intracranial lesions, 38% of patients achieved or exceeded intracranial remission for 12 months, comparable to that of the prior treatment group, demonstrating the durable effect of treatment on brain metastases in treatment-naïve patients.

What are the drug interactions of Selpercatinib?

When using Selpercatinib, be aware of the following drug interactions, which are important for the patient's treatment process.

1. Strong and moderate CYP3A inducers

Concomitant use with strong or moderate CYP3A inducers reduces plasma concentrations of Selpercatinib and may weaken the antitumor effect of the drug. Avoid this combination of medications. If unavoidable, the regimen of Selpercatinib should be adjusted to maintain the response to treatment.

2. CYP2C8 and CYP3A substrates

Selpercatinib is a moderate CYP2C8 inhibitor and a weak CYP3A inhibitor. When used with these substrate drugs, it may increase the plasma concentration of the substrate and increase the risk of adverse effects. If used with these drugs, it is recommended to follow the label of the substrate drug for dose adjustment and closely monitor for associated adverse effects.

What are the indications for Selpercatinib?

The main indications for Selpercatinib include the following cancer types, please refer to the label for details.

1. Treatment of cholangiocarcinoma

Selpercatinib can be used for specific cholangiocarcinomas, including those with inoperable advanced or metastatic cases. Patients should have FGFR2 fusions or other FDA-approved genetic rearrangement features.

2. Medullary/lymphoma with FGFR1 rearrangement

For adult patients, Selpercatinib can be used for relapsed or refractory myeloid/lymphoid tumors, particularly those with FGFR1 rearrangements.

[Warm tips] Before starting any new medication or supplement, inform your doctor or pharmacist about the medication you are currently taking to avoid possible drug interactions.