molecules of the month

VIP152 (BAY 1251152)

>50x family-selective CDK9 kinase inhibitor

IV agent (5-30 mg QW) in Ph. I for cancer

scaffold hop from atuveciclib

Journal of Medicinal Chemistry

Bayer, Berlin, DE / Vincerx, Palo Alto, US

Chemical structure of the VIP152 (BAY 1251152) inhibitor
1 min read

The Vincerx Pharma/Bayer CDK9 inhibitor, VIP152 (BAY 1251152), is a once-weekly (5-30 mg) IV agent in Ph. I for cancer with >50x family-selectivity. The sulfoximine-containing molecule is derived from the oral candidate atuveciclib (interestingly with opposite sulfoximine stereochemistry) and is significantly more potent under high ATP conditions. To maximize the therapeutic index, the team targeted a short half-life molecule to enable acute CDK9 inhibition for antitumor activity without prolonged transcription inhibition (oncogenic shock), with IV administration to reduce exposure variability. Solubility is key to IV administration, and the pyridine of VIP152 allowed it to have comparable solubility to atuveciclib at pH 4 (within the physiologically acceptable range for IV administration in humans), while the improved potency enabled a low IV dose. A…

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