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ARQ 501

ArQule, Inc.

Drug Names(s): ARQ 501

Description: The E2F transcription factor family of proteins is involved in the complex processes of both cellular proliferation and apoptosis . E2F is needed for cellular proliferation, however high levels of activated E2F or failed down-regulation of E2F can also trigger apoptosis through p53-dependent or -independent mechanisms. The activity of E2F is regulated through its interaction with the retinoblastoma (pRb) family of proteins which, when phosphorylated, release E2F, allowing it to transcribe E2F-responsive genes.

ARQ 501 is an E2F modulator that has demonstrated in preclinical studies potency and selectivity in the activation of faulty cellular checkpoint machinery in cancer cells. ARQ 501 activates E2F-mediated checkpoints leading to selective apoptosis (programmed death) of cancer cells. The compound also has demonstrated anti-cancer activity in mice when applied as both a single agent and in combination with certain chemotherapeutics.

Deal Structure: In April 2004, Roche obtained an option to ArQule's E2F program in the field of cancer therapy. Roche will provide immediate research funding of $15 million, and significant financial support for ongoing research and development. ArQule will be responsible for advancing drug candidates from early stage development into phase II trials. Roche may opt to license worldwide rights for the development and commercialization of products resulting from this collaboration, by paying an option fee. Assuming the successful development and commercialization of a compound under the program, ArQule could receive up to $276 million in payments, plus royalties. Additionally, ArQule has the option to co-promote products in the US.

In January 2009, Roche notified ArQule that it does not intend to exercise its option to license the E2F program, and hence Roche's rights to develop and commercialize candidates under the agreement will terminate as of the end of the year.

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