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Our Science

Leaders in Precision Oncology

Square blocks don’t fit in round holes. Why should drug development be any different?

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We design our drug candidates so they’re able to fit precisely where they’re supposed to fit. It’s a simple concept, yet complex to accomplish. The result is precision oncology: drugs designed with the sole purpose to block a specific cell-signaling pathway that leads to cancer progression.

Medicinal Chemists. Structure-based Drug Designers. Medicine Makers.

At Turning Point, we are focused on the cell signaling pathways that sit at the crux of uncontrolled cell growth and proliferation. Our macrocycle platform is the foundation of our current drug candidates. Our team of scientists and drug developers is applying novel small molecule design approaches integrating tumor biology and structure-based drug design to develop a new generation of orally available proprietary targeted agents that we believe will have the potential to address important unmet medical needs for patients.

We anticipate our internal and external exploration of oncology candidates will continue to include kinome targets and other oncogenic signaling proteins and pathways that address high unmet medical needs.

Designed to Be Different

Kinases are the proteins essential to cell-signaling processes that are necessary for normal cellular function. When mutations occur, these processes go awry and can lead to unchecked cell growth – a hallmark of cancer. While kinase inhibitors have been successful in blocking these cancer pathways, many are large and bulky, which makes them susceptible to certain resistant mutations.

Our drug candidates are designed to be different from conventional kinase inhibitors. From our core strengths in chemistry and structure-based drug design –a deep understanding of the shape and space of drug targets –we have designed kinase inhibitors to have a custom fit. In creating new molecules that are smaller and more compact, we have created a pipeline of kinase inhibitors that we believe may have the ability to maintain or enhance inhibition of the targeted kinase.

How it Works

To trigger signaling, kinases use a critical molecule for cell energy and growth, called ATP. This is why inhibitors of kinase proteins are designed to occupy the ATP binding pocket: they block this interaction and prevent oncogenic signaling.

We have designed our kinase inhibitors in our current pipeline to fit tightly into the ATP binding pocket, yet remaining unaffected by solvent-front, gatekeeper or compound resistance mutations: the genetic changes that enable cancer to circumvent treatment.

Turning Point Therapeutics is now a
Bristol Myers Squibb company

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