U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 161 - 170 of 3521 results

Status:
Investigational
Source:
NCT00942825: Phase 2 Interventional Completed Metastatic Non-squamous Non Small Cell Lung Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

CBP-501 is a chemically modified duodecapeptide and an analog of M-phase inducer phosphatase 3 (CDC25C) that increase cisplatin influx into tumor cells through an interaction with calmodulin enhancing cisplatin cytotoxicity, and affects cell cycle progression by abrogating DNA repair at the G2 checkpoint. CBP501 selectively inhibits the kinases MAPKAP-K2, C-TAK1, and CHK1 in vitro. Cell lines exposed to CBP501 plus bleomycin show a dose-dependent reduction of phosphorylated Ser216 on CDC25C. In addition to these effects on the G2 checkpoint, CBP501 also increases platinum concentration and DNA-platinum adduct formation in tumor cells through binding with calmodulin. In an in vitro panel testing the sensitivity of several tumor-derived cell lines to CBP501 in combination with a variety of anti-cancer agents, the combination of CBP501 with cisplatin was particularly effective against all four mesothelioma cell lines tested. Unfortunately, CBP-501 does not improve the efficacy of standard chemotherapy for malignant pleural mesothelioma.
Status:
Investigational
Source:
INN:delmitide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Delmitide is the decapeptide with antiinflammatory activity. It is the first low molecular weight compound inhibiting TNF production at a translational level. Also, delmitide inhibits production of IFN-gamma, IL-12 and IL-2. It targets TRAF6/IRAK4/MyD88 complex and inhibits phosphorylation of SAPKs (p38 and JNK). Delmitide inhibits AP1 and NFkB activation. Delmitide was developed for the potential treatment of Crohn's disease and ulcerative colitis; phase II trials for both these indications commenced in October 2001. Phase I trial in chemotherapy-induced diarrhea and the gastrointestinal complications of HIV were also initiated. However, no recent development has been reported.
Status:
Investigational
Source:
USAN:Azaline B
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Prazarelix is gonadorelin (GnRH) antagonist. It is primarily used in assisted reproduction to control ovulation. The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
Status:
Investigational
Source:
NCT01252693: Phase 2 Interventional Completed Prostate Cancer
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ozarelix is a luteinizing hormone-releasing hormone (LHRH) antagonist. It is known that LHRH antagonist exerts rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones. Thus this inhibitor can be effective in a variety of hormonally dependent disease including prostate cancer, benign prostatic hyperplasia (BPH), and endometriosis. Ozarelix was developed for the treatment of all these diseases including Alzheimer's disease. However, in January 2010 Spectrum Pharmaceuticals announced that it was discontinuing development of ozarelix in BPH. Because the low-dose intermittent therapy was disappointing in the treatment of lower urinary tract symptoms in men with BPH. The development of the drug for Alzheimer's disease was also discontinued. Ozarelix completed phase II trials for the treatment of prostate cancer and is in preclinical trials for the treatment of endometriosis and ovarian cancer.
Status:
Investigational
Source:
NCT03645434: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03773133: Phase 1/Phase 2 Interventional Terminated Small Cell Lung Cancer and Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:lutrelin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lutrelin is an agonist of gonadotropin-releasing hormone receptor exerting antineoplastic properties.
Status:
Investigational
Source:
NCT01612676: Phase 2 Interventional Completed Septic Shock
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Selepressin (FE 202158) was designed as a selective and short-acting vasopressin type 1a receptor (V(1a)R) agonist. This drug was developed for the treatment of vasodilatory hypotension in shock. Selepressin successfully completed phase IIa clinical trial, where was found that in septic shock patients, selepressin 2.5 ng/kg/minute was able to rapidly replace norepinephrine, improve fluid balance and shorten the time of mechanical ventilation.
Status:
Investigational
Source:
INN:detirelix
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Detirelix is a synthetic decapeptide containing five D-amino acids. It is a very potent Gonadotropin-releasing hormone (GnHR) antagonist. The acute effects of detirelix were consistent with peripheral vasodilation. Subchronic effects were associated with inhibition of pituitary gonadotropic and gonadal hormone secretion. As long-acting GnRH antagonist detirelix can rapidly suppress gonadotropin secretion, inhibit follicular development, and prevent ovulation. It can be used as luteolytic agent. A projected use is for the treatment of sex hormone-releasing diseases, as part of anticancer hormone therapy of sex-hormone-dependent tumors.