How Do RET Kinase Inhibitors Work?

Rearranged during transfection (RET) kinase inhibitors are a class of drugs used to treat nonsmall cell lung cancer and thyroid cancer that is either advanced or metastatic in people with tumors that have an alteration (mutation or fusion) in RET gene.

Enhanced RET oncogene expression is a hallmark of many cancers, including NSCLC and thyroid cancer. RET inhibitors are targeted therapies that act on tumors with activating alterations in the RET proto-oncogene, such as point mutations or fusions.

RET kinase inhibitors are administered via oral route, typically twice daily with or without food.

RET kinase inhibitors work in the following ways:

• They belong to a class of medications called "kinase inhibitors" that work by blocking kinase (an enzyme) that helps prevent cancer cells from growing and spreading to other parts of the body.
• They exert anti-tumor activity in specific cancers through the inhibition of mutated forms of RET tyrosine kinases.

RET kinase inhibitors are used to treat metastatic RET fusion-positive non-small cell lung cancer and advanced or metastatic RET-mutant medullary thyroid cancer.

Some of the common side effects include:

• Nausea
• Vomiting
• Constipation
• Diarrhea
• Headache
• Abdominal pain
• Tiredness/weakness
• Decreased appetite
• Dry mouth
• Stomatitis 
• Dysgeusia (taste disorder that causes foul, rancid, metallic, or salty taste perception)

Other rare side effects include:

• Dizziness 
• Fatigue 
• Rash/itching
• Anemia (low red blood cell count)
• Shortness of breath
• Chills, sore throat, fever, or cough
• Thrombocytopenia (low blood platelet count)
• Hypophosphatemia (low blood phosphate level)
• Hypertension (high blood pressure)
• Swelling of the hands, feet, legs, or ankles
• Increased liver enzymes
• Increased creatinine 
• Hypocalcemia (low blood calcium level)
• Hyponatremia (low blood sodium level)
• Peripheral neuropathy (damage to one or more groups of nerves)
• Hyperglycemia (high blood glucose level)

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of RET kinase inhibitors include:

• Gavreto
• Pralsetinib
• Retevmo
• Selpercatinib