This phase 1 study of quarfloxin (CX-3543) is designed to test the safety, tolerability, and highest safe dose of this drug when administered intravenously weekly for three weeks of a four week cycle in patients with advanced solid tumors.
Quarfloxin is a first-in-class small-molecule targeted cancer therapeutic derived from the validated fluoroquinolone class of drugs. Quarfloxin was rationally designed to target a G-quadruplex (QPLX) DNA structure and disrupt protein-DNA interactions essential to cancer cells. The QPLX targeted by quarfloxin forms within ribosomal DNA (rDNA) and the QPLX is bound by the nucleolin protein.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
Escalating doses of quarfloxin administered intravenously for 24 hours once weekly for three weeks every four weeks
Unnamed facility
Scottsdale, Arizona, United States
Unnamed facility
San Antonio, Texas, United States
Maximum tolerated dose (MTD) and Dose limiting toxicity (DLT)
Time frame: Cycle 1
Recommended Phase 2 dose
Time frame: Cycle 1
Pharmacokinetics (PK) in humans of intravenously administered quarfloxin
Time frame: One month
Evaluation of antitumor activity of quarfloxin by objective radiologic assessment
Time frame: Every 2 months
Pharmacodynamic evaluation of antitumor activity
Time frame: Monthly
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