Texaphyrin-Pt(IV) Conjugates and Formulations that Overcome Platinum Resistance
Life Sciences : Therapeutics
Available for licensing
- Jonathan Sessler, Ph.D. , Chemistry and Biochemistry
- Jonathan Arambula, Ph.D. , Chemistry and Biochemistry
- Zahid Siddik , University of Texas MD Anderson Cancer Center
- Gregory Thiabaud , University of Texas at Austin
- Greg Lyness , University of Texas at Austin
- Alan Watts , Drug Dynamics Institute - College of Pharmacy
Current FDA-approved platinum anticancer agents suffer from reduced uptake in addition to an inability to activate apoptosis through p53-mediated pathways. Of the FDA-approved platinum drugs, only oxaliplatin (Eloxatin®) is capable of addressing these molecular mechanisms of cancer resistance; however, it suffers from reduced drug uptake due to undesirable interactions with biological nucleophiles. Clearly, better formulations of oxaliplatin and other platinum anticancer agents are needed.
Researchers at The University of Texas at Austin have recently developed two texaphryin-platinum drug conjugates that address the problem of uptake and resistance. The conjugates were found to be significantly more cytotoxic than cisplatin in resistant ovarian cancer models. The conjugates are capable of delivering more platinum to the resistant cancer cells than any FDA-approved platinum agent. Initial studies in mice have shown that the animals are much more tolerant to the conjugates than towards other platinum-derived agents and that the conjugates show promise for further development and drug trials.
- Improved drug stability
- Improved drug solubility
- Improved drug uptake
- Effective towards platinum resistant cancers
- Less toxic than oxaliplatin and yet more efficacious in tumor reduction
- Controlled platinum release
- Ease of synthesis
These agents have been shown to be effective in both platinum resistant ovarian and lung cancer models but also may have utility in treating other types of cancers.
- 14 foreign patents application filed
- 1 foreign patent issued
- 1 U.S. patent application filed