Columbia Technology Ventures

Small molecule PI3K inhibitors for treating T-cell acute lymphoblastic leukemia

This technology is collection of small molecule PI 3-kinase (PI3K) inhibitors for treating T-cell acute lymphoblastic leukemia (T-ALL).

Unmet Need: Method for treating T-ALL by inhibiting PI3K

Current methods for treating T-ALL are limited, with only a few harsh treatments available to patients. In many cases T-ALL is caused by a loss of function of the tumor suppressor gene PTEN, leading to hyperactivation of PI3K. Two PI3K isoforms, gamma and delta, are sufficient to drive leukemogenesis in the absence of PTEN. CAL-130, a small molecule inhibitor of PI3Kγ/δ, was recently identified as a potential treatment for T-ALL, based on its ability to induce apoptosis in T-ALL cells and prolong survival in T-ALL mice. However, while CAL-130 is an encouraging therapeutic, it is not currently approved for treatment of T-ALL.

The Technology: Potent and effective inhibition of PI3K gamma and delta for treating cancer

This technology presents eight small molecule PI3K gamma and delta inhibitors for treating T-ALL. These small molecules all have similar activities to CAL-130, but have different molecular structures. As such, these compounds have demonstrated potency in killing cancer cells, with some compounds exhibiting higher activity than CAL-130. As a result, this cohort of diverse PI3K gamma and delta inhibitors has the potential to be developed into improved, effective treatments for cancers such as aggressive or relapsed T-ALL and other diseases associated with aberrant PI3K or PTEN activity.

This technology has been validated in vitro using cultured T-ALL cells.

Applications:

  • Treatment for T-ALL
  • Treatment for diseases linked with PI3K overactivity
  • Tool for inhibiting PI3Kγ/δ activity in PI3K/Akt signaling research

Advantages:

  • Range of related compounds with varied treatment response
  • Compound is structurally distinct from current CAL-130 inhibitor
  • Improved drug activity

Lead Inventor:

Donald Landry, Ph.D.

Patent Information:

Patent Issued

Related Publications:

Tech Ventures Reference: