The Food and Drug Administration (FDA) has granted Fast Track designation to sapanisertib for the treatment of adults with unresectable or metastatic squamous non-small cell lung cancer (sqNSCLC) whose tumors have a mutation in nuclear factor erythroid 2-related factor (NRF2) and who have received prior platinum-based chemotherapy and immune checkpoint inhibitor therapy.

Sapanisertib is a dual mTORC 1/2 inhibitor that targets a key survival mechanism in KEAP1/NRF2-mutated tumor cells. The designation is supported by a recent investigator-initiated phase 2 clinical trial ( Identifier: NCT02417701). Results showed that in heavily pretreated patients with NRF2-mutated sqNSCLC, treatment with sapanisertib was associated with an overall response rate of 27% (n=3/11) and median progression free survival of 8.9 months (95% CI, 7 months – not reached).

The Company is currently evaluating sapanisertib as monotherapy treatment in an open-label phase 2 trial ( Identifier: NCT05275673) in patients with NRF2-mutated sqNSCLC whose disease has progressed on or after platinum-doublet chemotherapy and immune checkpoint inhibitor therapy (anti-PD/L1) with or without anti-CTLA-4. 

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“While there have been significant advances in targeted treatments for lung cancer, little progress has been made specifically for patients with squamous lung cancer. In addition, we know that patients with lung cancers that harbor mutations in the NRF2/KEAP1 pathway typically have poorer outcomes than those whose tumors do not have these mutations,” said Susan Molineaux, CEO of Calithera. “This Fast Track designation allows for a variety of benefits, including the possibility of priority review of sapanisertib as we seek to provide a first-in-class treatment option that may help address the major unmet need in this patient population.”


Calithera receives FDA Fast Track designation for sapanisertib for the treatment of nrf2-mutated squamous lung cancer. News release. Calithera Biosciences, Inc. Accessed October 3, 2022.

This article originally appeared on MPR