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Version: 17.06d (Release date: 2017-06-26)
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Beta-lapachone Prodrug ARQ 761 (Code C99146)

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Terms & Properties

Preferred Name: Beta-lapachone Prodrug ARQ 761

Definition: A synthetic, soluble prodrug of beta-lapachone, a poorly soluble, ortho-naphthoquinone with potential antineoplastic and radiosensitizing activity. ARQ 761 is converted to beta-lapachone (b-lap) in vivo. When b-lap is activated by NAD(P)H:quinone oxidoreductase-1 (NQO1) this agent creates a futile oxidoreduction, generating highly reactive oxygen species (ROS) that results in DNA damage. The activation of b-lap also causes hyperactivation of poly (ADP-ribose) polymerase-1 (PARP-1), an enzyme that facilitates DNA repair, accompanied by rapid depletion of NAD+/ATP nucleotide levels. As a result, a caspase-independent and endoplasmic reticulum (ER) stress-induced mu-calpain-mediated cell death occurs in NQO1-overexpressing tumor cells. In addition, b-lap induces expression of the checkpoints activator E2F transcription factor 1 (E2F1) and thereby activates the E2F1-mediated checkpoint pathway that directly triggers apoptosis. As ARQ 761 is soluble and requires less solvent, this formulation may cause less hemolytic anemia associated with administration of the synthetic b-lap ARQ 501.

Display Name: Beta-lapachone Prodrug ARQ 761

Label: Beta-lapachone Prodrug ARQ 761

NCI Thesaurus Code: C99146 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL432960  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
ARQ 761
Beta-lapachone Prodrug ARQ 761

External Source Codes: 
PDQ Closed Trial Search ID 715599
PDQ Open Trial Search ID 715599 (check for NCI PDQ open clinical trial info)

Other Properties:
     Name Value (qualifiers indented underneath)
code C99146
Contributing_Source CTRP
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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