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CompletedNCT00524524Updated Oct 19, 2011

An Exploratory Biomarker Study of ARQ 501 in Patients With Advanced Solid Tumors

A Phase 1 interventional study of ARQ 501 in Advanced Solid Tumors, sponsored by ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA). Completed at 1 site in United States. Open to participants aged 18 Years and older. Per ClinicalTrials.gov, last updated 2011-10-19.

Sponsored by ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA) · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
9
Allocation
Non-randomized
Ages
18 Years and older
Sex
All
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Study summary

This study is designed to evaluate the response of several biomarkers in patients treated with ARQ 501. The results of the study may help the sponsor understand the effect of the study drug on these biomarkers and their respective role in cancer growth control.

Read the detailed description

ARQ 501 is an investigational anticancer agent that consists of a fully synthetic small molecule version of β-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho[1,2-b]pyran-5,6-dione) in a stable formulation for intravenous (IV) administration. ARQ 501 selectively induces apoptosis in cancer cells by the direct activation of the cellular checkpoints without damaging deoxyribonucleic acid (DNA) or microtubules. This therapeutic approach is known as Activated Checkpoint Therapy (ACT)sm. ACTsm is a novel strategy for treating and preventing cancers. Cell cycle checkpoints constitute an internal surveillance system that detects cellular, especially genetic, damage and either allows the cells to repair the damage, or induces apoptosis when damage is not repairable. Cancer cells are selectively eliminated upon checkpoint activation due to presence of irreparable DNA damage. It is believed that the rapid and selective induction of apoptosis in cancer cells by ARQ 501 is caused by a correspondingly rapid and sustained increase of the pro-apoptotic protein E2F1.

Preclinical studies have shown that exposure to ARQ 501 results in the activation or inactivation of a panel of 5 biomarkers. Time course changes in human tumor xenograft biomakers in athymic mice after exposure to ARQ 501 can be classified into 3 biomarker groups: those that changed shortly after exposure and returned to normal within 24 hours; those that changed shortly after exposure and remained for 24 hours or longer; and those that changed after 24 hours or later.

The primary objective is to evaluate the response of biomarkers in patients treated with ARQ 501. The exploratory study will help to illuminate the pharmacodynamics of these biomarkers, their roles in the cancer growth control, and their potential predictive or prognostic values for the disease and treatment of ARQ 501 in humans.

02

Conditions studied

  • Advanced Solid Tumors

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Keywords

  • solid tumors
  • biopsy
03

In context

Neoplasms

9,365 studies on the registry are indexed under Neoplasms; 2,489 are open to participants now.

This study's enrollment of 9 is below the median of 50 across 7,253 interventional studies indexed under Neoplasms.

Browse Neoplasms studies →

Lead sponsor

ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA) is the lead sponsor of 32 studies on the registry; none are open to participants now.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years and older
Sexes eligible
All
Accepts healthy volunteers
No

Inclusion criteria

  1. Able to provide signed and dated informed consent prior to study-specific screening procedures.
  2. Patients must have histologically or cytologically confirmed advanced solid tumor(s).
  3. Measurable disease as defined by RECIST (see Section 9.0).
  4. Patients must have Karnofsky performance status (KPS) ≥ 70%.
  5. Male or female patients of child-producing potential must agree to contraception or avoidance of pregnancy measures during the study and for 30 days after the infusion of ARQ 501.
  6. Females of childbearing potential must have a negative serum pregnancy test within seven days prior to the administration of study drug.
  7. ≥ 18 years old.
  8. Hemoglobin ≥ 10 g/dL
  9. Absolute neutrophil count (ANC) ≥ 1.5 x 10 9/L (≥1,500/mm3).
  10. Platelets ≥ 100 x 10 9/L (≥ 100,000/mm3).
  11. Total bilirubin ≤ 1.5 x upper limit of normal (ULN) or ≤ 3.0 x ULN with metastatic liver disease.
  12. Aspartate aminotransferase (AST) and alanine aminotransferase (ALT) ≤ 2.5 x ULN or ≤ 5.0 x ULN with metastatic liver disease.
  13. Creatinine ≤ 1.5 × ULN

Exclusion criteria

Exclusion Criteria:

  1. Active, uncontrolled systemic infection considered opportunistic, life threatening or clinically significant at the time of treatment
  2. Received anticancer chemotherapy, immunotherapy, radiotherapy, surgery or investigational agents within four weeks of first infusion
  3. Symptomatic or untreated central nervous system (CNS) involvement
  4. Previous exposure to ARQ 501
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Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Non-randomized
Intervention model
Single group
Masking
None (open label)
Enrollment
9 participants (actual)

Interventions

  • DrugARQ 501

    Weekly IV Infusion; 450 mg/m2

06

What researchers measure

Primary outcomes

  1. To evaluate the pharmacodynamics of a panel of biomarkers following administration of ARQ 501

    Time frame: Up to 30 hours after a single dose of ARQ 501

Secondary outcomes

  1. To further characterize the safety and tolerability of ARQ 501

  2. To assess anti-tumor activity of ARQ 501

07

Study locations

1 site
  • Dana Farber Cancer Institute
    Boston, Massachusetts 02115, United States
08

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Oct 19, 2011, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
09

Registry details

Key details

Study ID
NCT00524524
Lead sponsor
ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)
Responsible party
Sponsor
First posted
Sep 3, 2007
Start date
Aug 2007
Primary completion
Aug 2008
Completion
Aug 2008
Last update
Oct 19, 2011

Study contacts

Geoffrey Shapiro, MD, PhD
principal investigator · Dana-Farber Cancer Institute

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

Not currently enrolling

This study is completed, as verified in Oct 2011. You cannot join it, but the record below documents what was studied.

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Other studies in this condition

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Other studies from this sponsor

ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)

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