Temsirolimus

Drug · 2 studies in the Atlas

Intravenous rapamycin ester (CCI-779); mTOR inhibitor approved for advanced renal cell carcinoma.

Another clinical rapamycin derivative. An injectable, water-soluble version of rapamycin. It's an approved mTOR-blocking treatment for advanced kidney cancer.

CCI-779; a prodrug converted to sirolimus. Its RCC approval rests on the ARCC trial.

TL;DR. Temsirolimus appears in 2 curated studies in Oliver's mTOR Atlas: 1 in people (1 human study); 1 in animal models. It has 2 interactions in the curated pathway model.

Which mTOR drugs are in development now, and why: mTOR drugs in development →

In the pathway model

2 interactions in the curated mTOR pathway model. Each row is a claim with the evidence behind it; the evidence code is the kind of study, not its quality.

Interaction	Mechanism	Evidence	Studies
Temsirolimus inhibits mTORC1 mechanism: allosteric-inhibition · this link in full · on the map table	Temsirolimus is the IV version of rapamycin and, as far as we know, the first mTOR-blocking drug shown to help patients live longer in a controlled trial (in advanced kidney cancer). Temsirolimus is the intravenous rapamycin analogue, and, to our knowledge, the first mTOR inhibitor to show an overall-survival benefit in a randomised trial. Temsirolimus is the intravenous rapamycin analogue, and, to our knowledge, the first mTOR inhibitor to show an overall-survival benefit in a randomised trial. Holds under: HUD2007 shows the clinical effect (overall survival in poor-prognosis metastatic kidney cancer). It did not measure mTORC1 activity; that temsirolimus inhibits mTORC1 rests on the FKBP12-dependent mechanism it shares with rapamycin. shown in people · settled in the literature	H	HUD2007
Temsirolimus inhibits Renal cell carcinoma (RCC) mechanism: clinical-outcome · this link in full · on the map table	In hard-to-treat kidney cancer, temsirolimus helped patients live longer compared with an older drug. In poor-prognosis renal cancer, temsirolimus improved overall survival against interferon - the hardest endpoint there is. In poor-prognosis renal cancer, temsirolimus improved overall survival against interferon - the hardest endpoint there is. Holds under: Poor-prognosis patients specifically; the combination arm did not beat temsirolimus alone. shown in people · settled in the literature	H	HUD2007

Evidence at a glance

Evidence	What it means	Studies
H	Human study	1
A	Animal model	1

Studies

Year	Evidence	Study
2007	H	Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma HUD2007 Temsirolimus alone extended median overall survival to 10.9 months versus 7.3 months with interferon alfa in poor-prognosis metastatic kidney cancer; rash, hyperglycemia, and hyperlipidemia were more common with temsirolimus.
2026	A	SPOP-mediated ZMYND8 ubiquitination and phase separation exclusion drives mTOR inhibitor resistance in kidney cancer TAN2026 Identifies a mechanism of mTOR-inhibitor (everolimus/temsirolimus) resistance in clear cell renal cell carcinoma: SPOP-driven K63-linked ubiquitination of ZMYND8 excludes it from phase-separation compartments, enabling a ZMYND8-ZHX2 complex that drives NEK7 transcription and alternative p70S6K activation independent of mTOR inhibition. A NEK7-targeting PROTAC restored everolimus sensitivity in ccRCC cells and mouse tumors, nominating NEK7 as a target to overcome mTOR-inhibitor resistance.

Related entities

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Barton, O. (2026). Temsirolimus [Entity page]. In Oliver's mTOR Atlas [Data set]. https://mtor-atlas.org/drug/temsirolimus/ · Dataset DOI 10.5281/zenodo.22059963

@misc{atlas_drug_temsirolimus,
  author       = {Barton, Oliver},
  title        = {{Oliver's mTOR Atlas}: Temsirolimus},
  howpublished = {Entity page in a data set},
  year         = {2026},
  url          = {https://mtor-atlas.org/drug/temsirolimus/},
  doi          = {10.5281/zenodo.22059963}
}

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