Date: 2017-01-11
Type of information: Development agreement
Compound: PQR309
Company: Pierre Fabre Laboratories (France) Piqur Therapeutics (Switzerland)
Therapeutic area: Cancer - Oncology
Type agreement: development
Action mechanism:
- kinase ihibitor/mTOR inhibitor. PQR309 is an oral, brain-penetrant, dual inhibitor of the PI3K/mTOR pathway, which is activated in 60 – 80% of human cancers.
- PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
- As mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K, this agent may potentially be more potent than an agent that inhibits either PI3K kinase or mTOR kinase. By inhibiting mTOR to a lesser extent than PI3K, PQR309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy.
- PQR309 crosses the blood-brain barrier, expanding its use to malignant diseases involving the brain. Preclinical and Phase 1 studies have shown PQR309 to have a favorable safety,
tolerability and pharmacokinetic profile. In addition, PQR309 has shown both preclinical activity in various tumor models and clinical activity in Phase 1 and 2 studies. In November
2016, PQR309 was granted Orphan Drug Designation for PCNSL by the US FDA.
PQR309 is currently being investigated in five Phase 1 and 2 clinical studies in advanced solid tumors (NCT02483858), relapsed or refractory lymphoma (NCT02249429), relapsed or
refractory PCNSL (NCT02669511) and progressive glioblastoma multiforme (NCT02850744). In
addition, the PIQHASSO Phase 1/2b study investigates PQR309 in combination with Eisai’s Eribulin in metastatic HER2-negative and triple-negative breast cancer (NCT02723877).
Disease:
Details:
- • On January 11, 2017, PIQUR Therapeutics and Pierre Fabre announced that they have signed a collaboration agreement for the development of PIQUR’s lead compound PQR309 in dermato-oncology. The exclusive deal will see PIQUR and Pierre Fabre’s R&D teams work together on the evaluation and development of dermatological formulations of PI3K/mTOR inhibitors across multiple therapeutic indications.
- Following the first stage of the collaboration, Pierre Fabre will have the option to enter into exclusive negotiations to license global rights for the program in selected skin cancer conditions. Terms and conditions of the collaboration were undisclosed.
Financial terms:
Latest news:
Is general: Yes
