Clinical Trials

Tariquidar has been evaluated across several Phase 1, Phase 2, and Phase 3 clinical trials to assess its utility as a P-glycoprotein inhibitor and imaging agent. Sponsored by academic, government, and industry entities—including Washington University School of Medicine, the National Cancer Institute, and QLT Inc.—these primarily completed or terminated studies targeted non-small cell lung cancer, partial epilepsies, neuropathic pain, HIV-associated cognitive motor complex, and multidrug-resistant solid neoplasms. Notable research includes a completed Phase 1/2 investigation in neuropathic pain and Phase 3 trials combining Tariquidar with frontline chemotherapy for non-small cell lung carcinoma.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04603066 COMPLETED
Neuropathic Pain
Washington University School of Medicine
 2021-01-31 PHASE1; PHASE2
NCT03809234 TERMINATED
Neuropathic Pain
Washington University School of Medicine
 2019-05-20 PHASE1
NCT00082368 COMPLETED
Cancer
National Cancer Institute (NCI)
 2004-05-16 PHASE2
NCT01663545 Completed
Epilepsies Partial
National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)
 2012-07-31 --
NCT01547754 Terminated
HIV-Associated Cognitive Motor Complex
National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC)
 2012-01-09 --
NCT01386476 Completed
Drug Resistance
National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC)
 2011-06-15 --
NCT00069160 COMPLETED
Lung Neoplasms; Ovarian Neoplasms; Cervix Neoplasms; Renal Neoplasms
National Cancer Institute (NCI)
 2003-09 PHASE2
NCT00071058 COMPLETED
Adrenal Cortex Neoplasms
National Cancer Institute (NCI)
 2003-10 PHASE2
NCT00011414 COMPLETED
Wilms' Tumor; Sarcoma; Adenaocortical Carcinoma; Refractory Cancer; Coldrhood Cancer
National Cancer Institute (NCI)
 2001-02-15 PHASE1
NCT00082368 Completed
Cancer
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 2004-05-16 Phase 2
NCT00042302 TERMINATED
Stage IIIb Non-small Cell Lung Cancer; Stage IV Non-small Cell Lung Cancer
QLT Inc.
 2002-06 PHASE3
NCT00042315 TERMINATED
Stage IIIb Non-small Cell Lung Cancer; Stage IV Non-small Cell Lung Cancer
QLT Inc.
 2002-06 PHASE3
NCT00048633 COMPLETED
Breast Neoplasms
QLT Inc.
 2001-11 PHASE2

(data from https://clinicaltrials.gov, updated on 2025-08-14)

Check the Tariquidar (XR9576) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tariquidar binds noncompetitively to P-glycoprotein with high affinity (Kd = 5.1 nM), potently blocking ATP-dependent drug efflux transport and restoring intracellular chemotherapeutic accumulation in multidrug-resistant cells. By inhibiting membrane efflux transporter function to reverse drug resistance, tariquidar sensitizes resistant cells to cytotoxic agents in clinical conditions such as advanced non-small cell lung cancer and refractory solid tumors.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.