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

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Showing 671 - 680 of 13408 results

Status:
Investigational
Source:
NCT04638387: Not Applicable Interventional Terminated Osteoarthritis, Knee
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Withaferin A is one of the most bioactive phytoconstituents of Withania somnifera, a well-known herb in Ayurvedic medical tradition of India. Due to the lactonal steroid's potential to modulate multiple oncogenic pathways, Withaferin A has gained much attention as a possible anti-neoplastic agent. Systematic research on the evaluation of anticancer activities of withaferin A was started around the 1970s. Since then, a large number of studies have demonstrated the ability of withaferin A to suppress the in vivo growth of various human cancer cells’ xenograft tumors as well as experimentally induced carcinogenesis in different rodent models. It has being reported that withaferin-A reduced the growth of human prostate cancer (PC3) cells tumor xenograft in nude mice by blocking the tumor angiogenesis and inducing intratumoral apoptosis. According to this study, i.p. administration of withaferin-A caused regression of implanted tumor cells by decreasing the expression of angiogenesis marker CD31, inducing the expression of proapoptotic protein Bax, and activating caspase-3 via inhibition of nuclear factor-κB (NF-κB) signaling pathway. In a separate study, intratumoral administration of withaferin-A arrested PC3 cells’ xenograft tumor growth in mice by inducing tumor cell death via upregulation of prostate apoptosis response-4 (Par-4). Anticancer activity of withaferin-A has also being demonstrated for gynecological cancer, melanoma, thyroid, gastrointestinal and other types of cancer. Mechanistic basis of the anticancer effects of withaferin-A includes: (1) reinforcement of cellular antioxidant and/or detoxification system; (2) suppression of inflammatory pathways; (3) selective inhibition of tumor cell proliferation and induction of apoptosis; (4) suppression of tumor angiogenesis; (5) blockade of epithelial-to-mesenchymal transition (EMT), tumor invasion, and metastasis; (6) alteration of tumor cell metabolism; (7) immunomodulation; and (8) eradication of cancer stem cells.
Status:
Investigational
Source:
NCT04625595: Phase 1 Interventional Completed Type1 Diabetes
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

D-Methyldopa is an inactive isomer of methyldopa. It is known, that only L-isomer has the ability to inhibit dopa decarboxylase and possesses the antihypertensive activity in man. Moreover, about twice the dose of the racemate (DL-form of methyldopa) is required for the equal antihypertensive effect.
Status:
Investigational
Source:
NCT01927666: Not Applicable Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03189992: Phase 1 Interventional Unknown status Malignant Tumor of Small Intestine Metastatic to Liver
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cinobufotalin, the bufadienolide isolated from toad venom, has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane potential decrease, and reactive oxygen species (ROS) production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice daily, for 7 days) significantly inhibited A549 xenograft growth in mice. Further, same cinobufotalin administration improved mice survival at week five. Cinobufotalin administration didn’t significantly affect mice body weight, indicating the relative safety of this regimen. Thus, cinobufotalin inhibits A549 xenograft growth in vivo and improves mice survival.
Status:
Investigational
Source:
NCT03045861: Phase 2 Interventional Completed Infection, Human Immunodeficiency Virus
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT02653729: Phase 2 Interventional Completed Psychosis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04693000: Phase 2 Interventional Unknown status Keratotic Nodular Size
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Solasodine is an aglycone of solamargine and solasonine, which are the major solasodine glycosides present in numerous species of the solanaceae family including potato, tomato or garden egg plant etc. In Phase II clinical trial was shown that solasodine glycosides exhibit anticancer activity against skin cancer. The effects of aglycone solasodine on cancer cells have also been investigated. Solasodine inhibits the growth of human colon and liver cancer cell. In addition, solasodine effectively inhibits proliferation of HER2-overexpressing breast cancer cells and inhibits invasion of human lung cancer cells. Solasodine possesses CNS activities such as antipyretic, anticonvulsant and memory enhancing effects. Also, solasodine has been found to possess diuretic, antifungal, hepatoprotective, immunomodulatory, anti-spermatogenetic and antiandrogenic effects.
Status:
Investigational
Source:
JAN:VILAPRISAN [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Vilaprisan, a small molecule progesterone receptor antagonist is being developed by Bayer HealthCare Pharmaceuticals (formerly Bayer Schering Pharma) for the treatment of endometriosis and uterine leiomyoma. Hormonal imbalance observed in women with endometriosis is a potential target for treating endometriosis. Vilaprisan is a highly selective steroidal progesterone receptor modulator (SPRM). It is a partial agonist of progesterone receptor, which means that the drug activates progesterone receptors to a certain degree upon binding. This triggers a cascade of biochemical reactions that result in the suppression of prostaglandin production. This, in turn, relieves symptoms such as pain and bleeding. Modulating progesterone by taking vilaprisan might help in treating endometriosis over the long term. Phase I and II studies give encouraging results on the efficacy of vilaprisan at different doses. Like other SPRMs, vilaprisan induces benign changes of endometrium (PR modulator-associated endometrial changes, PAECs). These disappear as treatment is discontinued. Unlike GnRHa treatment, neither UPA nor vilaprisan induce hypoestrogenism and associated symptoms. Phase III studies are ongoing to confirm efficacy and safety of vilaprisan in long-term treatment of symptomatic fibroids.
Status:
Investigational
Source:
NCT04234100: Not Applicable Interventional Completed Blood Pressure
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


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

Class (Stereo):
CHEMICAL (ACHIRAL)