MTOR inhibitor

MTOR inhibitor
Drug class
Class identifiers
Use	Cancer treatment, immunosuppression
ATC code	L01
Biological target	mTOR

mTOR inhibitors are a class of drugs that inhibit the mechanistic target of rapamycin (mTOR), which is a serine/threonine-specific protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. mTOR inhibitors are used in the treatment of cancer and as immunosuppressants in organ transplantation.

Mechanism of Action

mTOR functions as part of two distinct complexes, mTORC1 and mTORC2, each of which has different roles in cell physiology. mTORC1 promotes protein synthesis by phosphorylating key regulators of mRNA translation and ribosome synthesis. Inhibition of mTORC1 leads to reduced cell proliferation and angiogenesis, making it a target for cancer therapy. mTORC2 is involved in the regulation of cell survival and acts on different downstream pathways.

mTOR inhibitors work by binding to the mTOR complex and disrupting its function. This inhibition reduces the activity of downstream effectors that are critical for cell cycle progression and growth.

Clinical Uses

mTOR inhibitors are primarily used in the treatment of various types of cancer, including renal cell carcinoma, subependymal giant cell astrocytoma, and pancreatic neuroendocrine tumors. They are also used in preventing the rejection of transplanted organs due to their immunosuppressive effects.

Examples of mTOR Inhibitors

• Sirolimus (also known as rapamycin)
• Everolimus
• Temsirolimus

Side Effects

Common side effects of mTOR inhibitors include mouth ulcers, rash, diarrhea, fatigue, and pneumonitis. More severe side effects can include non-infectious pneumonitis, hyperlipidemia, and hyperglycemia.

Research Directions

Research continues to explore the full potential of mTOR inhibitors in treating more types of cancer and other diseases where cell growth is dysregulated. Studies are also investigating the combination of mTOR inhibitors with other therapies to enhance efficacy and reduce resistance.

See Also

• Cancer therapy
• Immunosuppressive drug
• Protein kinase inhibitor