Difference between revisions of "Pimitespib (Jeselhy)"

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m (Jwarner moved page Pimitespib (TAS-116) to Pimitespib (Jeselhy): PMDA approval)
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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/pimitespib NCI Drug Dictionary]: A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, Hsp90alpha/beta inhibitor TAS-116 specifically binds to and inhibits the activity of Hsp90 alpha and beta; this results in the proteasomal degradation of oncogenic client proteins, which inhibits client protein dependent-signaling, induces apoptosis, and inhibits the proliferation of cells overexpressing HSP90alpha/beta.
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/pimitespib NCI Drug Dictionary]: A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, Hsp90alpha/beta inhibitor TAS-116 specifically binds to and inhibits the activity of Hsp90 alpha and beta; this results in the proteasomal degradation of oncogenic client proteins, which inhibits client protein dependent-signaling, induces apoptosis, and inhibits the proliferation of cells overexpressing HSP90alpha/beta.
  
==Preliminary data==
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==Diseases for which it is used==
===[[Gastrointestinal stromal tumor]]===
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*[[Gastrointestinal stromal tumor]]
#'''CHAPTER-GIST-301:''' Kurokawa Y, Honma Y, Sawaki A, Naito Y, Iwagami S, Komatsu Y, Takahashi T, Nishida T, Doi T. Pimitespib in patients with advanced gastrointestinal stromal tumor (CHAPTER-GIST-301): a randomized, double-blind, placebo-controlled phase III trial. Ann Oncol. 2022 Jun 8:S0923-7534(22)01718-5. Epub ahead of print. [https://doi.org/10.1016/j.annonc.2022.05.518 link to original article] [https://pubmed.ncbi.nlm.nih.gov/35688358/ PubMed] JapicCTI-184094
 
  
 
==Also known as==
 
==Also known as==
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[[Category:Hsp90 inhibitors]]
 
[[Category:Hsp90 inhibitors]]
[[Category:Gastrointestinal stromal tumor medications (investigational)]]
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[[Category:Gastrointestinal stromal tumor medications]]
 
[[Category:PMDA approved drugs]]
 
[[Category:PMDA approved drugs]]

Revision as of 17:35, 6 September 2022

Mechanism of action

From the NCI Drug Dictionary: A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, Hsp90alpha/beta inhibitor TAS-116 specifically binds to and inhibits the activity of Hsp90 alpha and beta; this results in the proteasomal degradation of oncogenic client proteins, which inhibits client protein dependent-signaling, induces apoptosis, and inhibits the proliferation of cells overexpressing HSP90alpha/beta.

Diseases for which it is used

Also known as

  • Code name: TAS-116
  • Brand name: Jeselhy