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NCI Drug Dictionary


doxorubicin-GnRH agonist conjugate AEZS-108  
A peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Doxorubicin-GnRH agonist conjugate AEZS-108 binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates into DNA and inhibits the topoisomerase II activity, which may result in the inhibition of tumor cell DNA replication and tumor cell proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

doxorubicin-HPMA conjugate  
A copolymer conjugate of the antineoplastic anthracycline doxorubicin and the water-soluble polymer N-(2-hydroxypropyl) methacrylamide (HPMA). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipid. HPMA conjugation enhances the permeability and retention of this agent within the tumor vasculature. Poorly cleared by the lymphatic system, this formulation undergoes increased cleavage by tumor cell lysosomal proteinases, resulting in increased, sustained intracellular concentrations of free doxorubicin. Compared to other doxorubicin-containing formulations, this formulation may exhibit an improved toxicity profile due to the lower concentrations of free doxorubicin to which non-malignant tissues are exposed. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

doxorubicin-magnetic targeted carrier complex  
A formulation of the anthracycline antibiotic doxorubicin in which doxorubicin is bound to microscopic beads of activated carbon and iron as a magnetic-targeted carrier (MTC). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipids. Guided by the placement of a magnet on the body surface overlying a tumor site, the doxorubicin-MTC complex delivers doxorubicin directly to the tumor site, thereby targeting and prolonging the duration of doxorubicin-mediated cytotoxicity to the tumor bed while minimizing systemic toxicity. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

doxycycline  
A synthetic, broad-spectrum tetracycline with antimicrobial activity. Doxycycline binds reversibly to the 30S ribosomal subunit and possibly to the 50S ribosomal subunit, blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex, which results in an inhibition of bacterial protein synthesis. In addition, this agent may inhibit collagenase activity. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

doxycycline hyclate  
The hyclate salt form of doxycycline, a synthetic, broad-spectrum tetracycline antibiotic exhibiting antimicrobial activity. Doxycycline hyclate binds reversibly to the 30S ribosomal subunit, possibly to the 50S ribosomal subunit as well, thereby blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This leads to an inhibition of protein synthesis. In addition, this agent has exhibited inhibition of collagenase activity. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

dronabinol  
A synthetic form of delta-9-tetrahydrocannabinol, a psychoactive substance found in Cannabis sativa. Dronabinol acts directly on the appetite and vomiting control centers in the brain to stimulate appetite and prevent emesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

droperidol  
A butyrophenone with anti-emetic, sedative and anti-anxiety properties. Although the exact mechanism through which droperidol exerts its effects is unknown, droperidol may block dopamine receptors in the chemoreceptor trigger zone (CTZ), which may lead to its anti-emetic effect. This agent may also bind to postsynaptic gamma-aminobutyric acid (GABA) receptors in the central nervous system (CNS), which increases the inhibitory effect of GABA and leads to sedative and anti-anxiety activities. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Droxia  
(Other name for: hydroxyurea)

DT(388)IL3 fusion protein  
A recombinant protein consisting of human interleukin 3 (IL3) fused to the first 388 amino acids of diphtheria toxin [DT(388)] with potential antineoplastic activity. Upon administration, the IL3 moiety of the DT(388)IL3 fusion protein binds to IL3 receptors on cells expressing the receptor. Subsequently, the DT(388) toxin moiety, containing both translocation and catalytic domains, translocates across the cell membrane endocytotically; within the cytosol, the catalytic domain catalyzes the ADP-ribosylation of, and inactivates, translation elongation factor 2 (EF-2), resulting in the inhibition of translation during protein synthesis. IL3 may be overexpressed by acute myeloid leukemia (AML) cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

DTA-H19 plasmid  
A plasmid DNA encoding the A chain of the diphtheria toxin (DT-A) driven by the transcriptional regulatory sequences of human H19, with potential antineoplastic activity. Because the expression of DT-A is under the control of H19 promotor elements, DT-A is selectively expressed in tumor cells capable of turning on H-19. DT-A catalyzes ADP-ribosylation of translation elongation factor 2 (EF-2), resulting in the inhibition of protein synthesis and apoptosis. In addition, DT-A protein released from lysed cells cannot enter and kill neighboring cells because of the absence of the DT-B chain, further enhancing the selective cytotoxicity of this agent. Human H19 is a paternally-imprinted, oncofetal gene encoding an RNA product; it acts as a "riboregulator" in gene expression and is found at substantial levels in different human tumor cell types while its expression in normal adult tissue is limited. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

DTIC-Dome  
(Other name for: dacarbazine)

dual ALK/EGFR inhibitor AP26113  
An orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Dual ALK/EGFR inhibitor AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. This leads to the inhibition of ALK kinase and EGFR kinase, disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells. In addition, AP26113 appears to overcome mutation-based resistance. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. EGFR is overexpressed in a variety of cancer cell types. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

dual PI3 kinase/mTOR inhibitor GDC-0980  
An orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor GDC-0980 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Dual PI3 Kinase/mTOR Inhibitor PKI-587  
An agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Upon intravenous administration, PI3K/mTOR kinase inhibitor PKI-587 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

duborimycin  
An anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Duborimycin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

dulanermin  
A recombinant human soluble protein corresponding to amino acids 114-281 of the Apo2 ligand/tumor necrosis factor-related apoptosis-inducing ligand (RhApo2L/TRAIL) with potential antineoplastic activity. Dulanermin binds to and activates TRAIL receptors 1 and 2 (TRAIL-R1/R2), which may activate caspases and induce p53-independent apoptosis in TRAIL-R1/R2-expressing tumor cells. The pro-apoptotic cell surface receptors TRAIL-R1 and -R2, also known as DR4 (death receptor 4) and DR5 (death receptor 5), are members of the TNF receptor family and are overexpressed by a variety of cancer cell types. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

duloxetine hydrochloride  
The hydrochloride salt of duloxetine, a fluoxetine derivative belonging to the class of selective serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors (SSNRIs) and exhibiting antidepressant activity. Duloxetine selectively prevents the reuptake of 5-HT and NE via transporter complexes on the pre-synaptic membrane, thereby increasing the level of these neurotransmitters within the synaptic cleft. As a result, this agent potentiates serotonergic and noradrenergic activities in the central nervous system, and alleviates depression and neuropathy sensations, such as pain and tingling. Furthermore, duloxetine does not show significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and gamma-aminobutyric acid (GABA) receptors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

dutasteride  
A synthetic 4-azasteroid compound with antiandrogenic activity. Dutasteride competitively and specifically binds to isoenzymes 1 and 2 of 5-alpha-reductase, forming stable enzyme complexes and inhibiting the conversion of testosterone to 5α-dihydrotestosterone (DHT); the reduction in DHT activity may mitigate or prevent enlargement of the prostate gland. The type 2 5-alpha-reductase isoenzyme is primarily active in the reproductive tissues while the type 1 isoenzyme is also active in skin and the liver. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Dynacin  
(Other name for: minocycline hydrochloride)

Dysport  
(Other name for: botulinum toxin type A)

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