Therapy Areas: Inflammatory Diseases
Exelixis, Aurigene Release Preclinical Data on Novel CDK7 Inhibitor
12 October 2020 - - US-based oncology-focused biotechnology company Exelixis, Inc. (NASDAQ: EXEL) and Indian development stage biotech company Aurigene Discovery Technologies Ltd have disclosed new preclinical data showing that AUR102 has potent anti-tumor activity in a large panel of cancer cell lines, the companies said.

AUR102 is a potent, selective, and orally bioavailable covalent inhibitor of cyclin-dependent kinase 7, which is an important regulator of the cellular transcriptional and cell cycle machinery.

Exelixis has an exclusive option for AUR102 under its July 2019 exclusive collaboration, option and license agreement with Aurigene.

The new data will be presented in a poster (Abstract 170) at the 32nd EORTC-NCI-AACR Symposium, which is being held virtually on October 24-25, 2020.

The abstract provides a summary of results from a detailed characterization of AUR102 in cancer cell lines and animal tumor models. Additional data will be presented in the poster.

Key findings included in the abstract are:

AUR102 exhibited potent anti-proliferative activity in a large panel of cell lines with induction of cell death in cell lines derived from multiple cancer types.

The observed anti-proliferative activity correlated with cellular CDK7 target engagement and decreased levels of P-Ser5 RNAPII, a key mediator of transcription.

AUR102 studies showed synergy when used in combination with multiple chemotherapies.

Oral dosing with AUR102 resulted in dose-dependent anti-tumor activity, including complete tumor regression in diffuse large B-cell lymphoma, acute myeloid leukemia, and triple-negative breast cancer xenograft models.

Inhibition of tumor growth was accompanied by complete target engagement as demonstrated in a parallel PK-PD study.

AUR102 significantly impacts several pathways and key cancer driver and immune-response genes.
The study authors conclude that the data support clinical evaluation of AUR102 as a single agent and in combination with chemotherapies for the treatment of cancer.

Under the terms of the July 2019 agreement, Exelixis made an upfront payment of USD10 m for exclusive options to license three preexisting programs from Aurigene.

In addition, Exelixis and Aurigene initiated three Aurigene-led drug discovery programs on mutually agreed upon targets, in exchange for additional upfront option payments of USD 2.5m per program.

Exelixis is also contributing research funding to Aurigene to facilitate discovery and preclinical development work on all six programs.

As the programs mature, Exelixis will have the opportunity to exercise an exclusive option for each program up until the time of Investigational New Drug filing acceptance.

If Exelixis decides to exercise an option, it will make an option exercise payment to Aurigene and assume responsibility for that program's future clinical development and commercialization including global manufacturing.

Aurigene will be eligible for clinical development, regulatory, and sales milestones, as well as royalties on sales.

Under the terms of the agreement, Aurigene retains limited development and commercial rights for India and Russia.

Aurigene is a development stage biotech company engaged in discovery and clinical development of novel and best-in-class therapies to treat cancer and inflammatory diseases and a wholly owned subsidiary of Dr. Reddy's Laboratories Ltd. (BSE: 500124) (NSE: DRREDDY) (NYSE: RDY).

The company is focused on precision-oncology, oral immune checkpoint inhibitors, and the Th-17 pathway.

Aurigene's programs currently in clinical development include an oral ROR-gamma inhibitor AUR101 for moderate to severe psoriasis in phase 2 under a US FDA IND and a PD-L1/ VISTA antagonist CA-170 for non-squamous non-small cell lung cancer in phase 2b/3 in India.

Additionally, Aurigene has multiple compounds at different stages of pre-clinical development. Aurigene has also partnered with several large and mid-pharma companies in the United States and Europe and has multiple programs in clinical development.


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