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PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. PQR309 is an mTORC1 and mTORC2 inhibitor.

PQR309 is a highly selective pan-PI3K inhibitor with a balanced targeting of mTOR kinase. PQR309 also inhibits PI3Kα-H1047R), PI3Kα-E542K and PI3Kα-E545K with IC50s of 36 nM, 63nM and 136 nM, respectively[1].

Oral administration yields similar concentrations of PQR309 in brain and plasma samples illustrates that PQR309 readily passes the blood-brain barrier. In mice, both po and iv application routes show a rapid drop below 200 ng/mL (~0.5 uM) of PQR309 within 50%). Twenty-four hours after po administration, plasma levels of PQR309 are still >2 uM (800-1000 ng/mL). Moreover, after 1-2 h exposure to PQR309, drug levels in rat brain samples are comparable to plasma levels, confirming rapid access of PQR309 to the brain[1].

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