1026 Targeted Degradation
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Product Development

What’s next for targeted protein degradation

As the technology goes mainstream, next-gen molecules will use new enzymes, tap new pathways, and address PK/PD challenges

As the technology goes mainstream, next-gen molecules will use new enzymes, tap new pathways, and address PK/PD challenges.

Oct 23, 2020 | 10:52 PM GMT

As targeted protein degradation grows up, the field is going after harder targets and new mechanisms of action.

Over the last year, a series of Phase I/II readouts from front-runner Arvinas Inc. (NASDAQ:ARVN), including the May 13 unveiling of the technology’s first efficacy signal, have taken targeted protein degradation from preclinical white space to clinically viable modality. More efficacy data are expected by year-end.

The company has shown its two lead candidates are well-tolerated and orally bioavailable, and that its androgen receptor degrader ARV-110 induced confirmed PSA declines of >50% in two out of eight castration-resistant prostate cancer (CRPC) patients previously treated with multiple lines of therapy; one of the patients showed a confirmed RECIST partial response. As of May 29, follow-up data had not found responses in four additional patients.

“It was a big de-risking event for the entire field,” Arvinas CSO Ian Taylor told BioCentury. Arvinas raised $238 million through its Sept. 2018 IPO and Nov. 2019 follow-on.

Almost all the major pharmas and

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