From our proprietary pipeline of >12,000 small molecules we have selected Myrtleciclib as lead compound, most active against CDK4/6/9 dependent tumors expressing Myc, such as mesothelioma, breast cancer, lymphomas and other aggressive cancers.
ViroStatics’ clinical candidate Myrtleciclib, in advanced preclinical development, displays a good druggability profile and some unique features:
- Unique mechanism of action: blocking Myc ensuring selective, non-competitive CDK9/6/4 inhibition
- Anti-proliferative activity against a broad spectrum of cancers, superior to comparators
- Inducing apoptosis and cell death, selectively on cancer cells
- Efficacy demonstrated for a number of cancers in disease relevant animal models, including CDK4/6i resistant cancers
- Broad therapeutic index with favorable toxicity profile in rodents and non-rodents
- Advanced preclinical stage, promising ADME, API GMP-ready, 18 months needed to complete IND enabling package. Potential back-up and follow-on compounds at earlier preclinical stage
The initial indication would be Malignant Pleural Mesothelioma (MPM) one of the most devastating cancers, with a life expectancy of 15-22 months. MPM, where CDK9 pathway plays an important role, has no targeted small molecules treatment options and represents a rare disease that could grant VS2-370 Myrtleciclib an orphan drug status and a fast-track regulatory approval. MPM market has been expanding in the last 20 years.
We have also activity data in vitro and in vivo supporting additional indications such as metastatic breast cancer and lymphomas, including those aggressive cancers that are CDK4/6i resistant.
Original Myrtleciclib patent protection has been granted in most countries and is planned to be extended up to 2043.