NCT01056029

Dose-Escalation Phase 1 Study of G-202 (Mipsagargin) in Patients With Advanced Solid Tumors

An Open Label, Single-Arm, Dose-Escalation Phase 1 Study of G-202 (Mipsagargin) in Patients With Advanced Solid Tumors

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 30 (estimated)
• Sponsor: GenSpera, Inc. · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

This is an open-label, single-arm, dose-escalation Phase I study to determine the maximum tolerated dose (MTD) of G-202 (mipsagargin) when administered once daily for 3 consecutive days of a 28-day cycle in patients with advanced solid tumors. G-202 will be administered by intravenous infusion over 1 hour on Days 1, 2 and 3 of each 28-day cycle.

Detailed description

Pro-drug chemotherapy is an approach to cancer treatment that is being investigated as a means to achieve higher concentrations of cytotoxic or biologically active agents at a tumor location while avoiding systemic toxicity. With pro-drug chemotherapy, a relatively non-toxic form of a cytotoxin, the pro-drug, is converted into the active cytotoxic agent at the tumor site or other specific location. G-202 (mipsagargin) is a thapsigargin pro-drug; it consists of a cytotoxic analog of thapsigargin coupled to a masking peptide which inhibits its biologic activity until proteolytic cleavage at the tumor site. Thapsigargin is a natural product with profound effects on cell viability. Thapsigargin is a non-cell-type specific toxin with documented ability to kill a broad spectrum of cancer cell lines as well as normal endothelial cells, fibroblasts and osteoblasts. It induces a rapid and pronounced increase in the concentration of cytosolic calcium, due to blockade of the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump to which it binds with high affinity. The increase in cytosolic calcium leads to induction of apoptosis and ensuing cell death. The anti-tumor effect of G-202 in humans with advanced solid tumors is not yet known.

Conditions

• Advanced Solid Tumors

Interventions

Type	Name	Description
DRUG	G-202	Thapsigargin is Pro-drug chemotherapy which will be administered by intravenous infusion over 1 hour on Days, 1, 2 and 3 of each 28 day cycle

Timeline

• Start date: 2010-01-01
• Primary completion: 2012-12-01
• Completion: 2013-08-01
• First posted: 2010-01-26
• Last updated: 2015-12-10

Locations

3 sites across 1 country: United States