Clinical Program

Lead Compound: Caplostatin™

The Company’s drug development strategy focuses first on cancer therapy. Our lead compound – Caplostatin™ - is in pre-clinical development for cancer. Caplostatin is the combination of two functional parts: a MetAP2 inhibitor clinically proven in over 300 cancer patients coupled to a bio-compatible polymer, cinically proven to improve safety, bio-distribution, tumor targeting, and pharmacokinetics of the attached drug. This rational drug model represents the next generation of targeted cancer therapy.

 

Lodamin   Lodamin micelle

SynDevRx is also developing Lodamin for cinical trials.  Early pre-clinical experiments showed substantial antitumor effects (83% reduction) in a lung cancer model. A similar antitumor effect of Lodamin was observed with melanoma B16/F10 tumors, confirming the broad biological effect of Lodamin, very much likethe original free TNP-470. TUNEL staining indicated a high level of tumor cell apoptosis after treatment.

One of the most important effects of oral Lodamin is the prevention of liver metastasis in mice. Liver metastasis is very common in many tumor types and is often associated with poor prognosis and survival.



Rational Drug Development

The concept is simple: small molecules are easier to manufacture and characterize than large proteins or monoclonal antibodies, but are indiscriminate in their targeting.  That makes them prone to cause a host of unwanted side effects. By conjugating (or attaching) the active small molecule to a large, bio-compatible co-polymer, the side effects are minimized.  An added benefit is that the HPMA co-polymer also acts as a tumor-targeting device. This technique has been clinically proven to increase the amount of drug delivery to the tumor site by more than 4X, increase drug half-life by as much as 14X, and improve the safety profile significantly.