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[Pharmacology](https://durgical.com/en/pharmacology/) · Class

# mTOR inhibitors

Drugs that block mTOR, a master switch of cell growth: used to prevent transplant rejection and to treat some cancers and rare lung and tumour diseases.

Updated 2026-11-01

## What they are

Rapamycin (sirolimus) and its derivative everolimus. Sirolimus prevents kidney transplant rejection and treats lymphangioleiomyomatosis; everolimus is used in transplantation and in cancers such as advanced breast cancer, kidney cancer and neuroendocrine tumours.

## Mechanism of action

Like tacrolimus, these drugs bind FKBP12 inside the cell, but the complex does not touch calcineurin. Instead it binds and inhibits mTOR, a kinase that links growth-factor and cytokine signals (such as IL-2) to cell-cycle progression and protein synthesis. T cells and tumour cells stall before entering the S phase.

Target: mTOR kinase (mTORC1), reached through FKBP12

## Key points

- They bind FKBP12 like tacrolimus, but inhibit mTOR, not calcineurin.
- Hyperlipidaemia (cholesterol and triglycerides) is very common.
- They impair wound healing and cause lymphocele, mouth ulcers and oedema.
- They cause proteinuria, and combined with calcineurin inhibitors they raise the risk of thrombotic microangiopathy.
- Interstitial pneumonitis is a recognised serious effect.

## Drugs in this class

- [**Sirolimus** A transplant drug (rapamycin) that blocks the mTOR growth switch in T cells. It raises cholesterol, slows wound… mTOR (mechanistic target of rapamycin), through FKBP12](https://durgical.com/en/pharmacology/sirolimus/)
- [**Everolimus** An oral mTOR inhibitor related to rapamycin, used for some breast, kidney and neuroendocrine cancers. Mouth sores… mTOR (mechanistic target of rapamycin), through FKBP12](https://durgical.com/en/pharmacology/everolimus/)

## Others in the class

- temsirolimus

## Test yourself

Think of the answer, then tap the question to see it.

## Sirolimus and tacrolimus both bind FKBP12. How do their targets differ?

The tacrolimus-FKBP12 complex inhibits calcineurin; the sirolimus-FKBP12 complex leaves calcineurin alone and inhibits mTOR.

## Why is sirolimus often delayed or avoided right after surgery in some transplant recipients?

It impairs wound healing and causes lymphocele and wound dehiscence.

## Which laboratory abnormality is especially common with mTOR inhibitors?

High cholesterol and triglycerides.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - SIROLIMUS solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f9843d49-0e16-4427-9cea-9f66f32b97f7) (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 39 (McGraw Hill, 2023).

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