01/28/2025
Eli Lilly made a bold move with this acquisition of a PI3Kα inhibitor, targeting breast cancer therapy and solid tumors. More options are coming available and the advances are downstream from the typical receptor tyrosine kinase inhibitors.
The PI3K protein is between the RTK and Akt, a centrally active signaling protein involved in the mTORC2 and mTORC1 pathway.
This pathway was the focus of my research on a naturally occurring chemical made by a mold, called Chaetoglobosin K, which does not inhibit PI3K.
Other therapies targeting this pathway include copanlisib, idelalisib, duvelisib, and umbralisib. However, these medications are not specific to the PI3Kα subunit of the protein.
The drug idelalisib was the first to be approved by the FDA in 2014. The only other PI3Kα inhibitor on the market is alpelisib, which was approved in 2019.
Inhibiting PI3K leads to an increase of estrogen receptor-dependent activity, therefore, fulvestrant has been approved with many of the treatments to dampen down the estrogen activation.
Why is this big?
- It's more targeted than previous therapies
- It advances beyond typical receptor tyrosine kinase inhibitors
- It could be a new weapon against aggressive cancers
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