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

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Showing 171 - 180 of 2243 results

Status:
Investigational
Source:
INN:cefuracetime
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefuracetime is an impurity of Cefuroxime, which is an antibacterial agent.
Status:
Investigational
Source:
INN:diphoxazide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diphoxazide is the anticonvulsant and psychosedative agent.
Status:
Investigational
Source:
INN:ramorelix
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ramorelix is a glycosylated gonadoliberin antagonist patented by Hoechst A.-G. as an anticancer agent. In preclinical studies, a single injection of ramorelix microparticles inhibited tumor progression for only 14 days. This short action is due to a different release profile of the ramorelix microparticles and the different specific activities of peptides incorporated. In the preventive experiments, animals were treated 17 days after DMBA induction before tumor development. Treatment with buserelin implants every 56 days or with buserelin microparticles every 28 days and the treatment with ramorelix microparticles every 7 days prevented the development of tumors. Six weeks after the last injection of ramorelix microparticles a strong tumor progression was seen. There was a clear correlation between peptide release and tumor inhibition. The implants and the microparticles were well tolerated, no tissue reaction or side-effects of ramorelix were seen.
Status:
Investigational
Source:
INN:loviride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Loviride (R 89439) is a non-nucleoside inhibitor of reverse transcriptase. It inhibits virion and recombinant reverse transcriptase of HIV-1. It was being studied in the combination therapy of HIV infection with other anti-HIV agents.
Status:
Investigational
Source:
INN:ozarelix [INN]
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:
NCT02204085: Phase 1/Phase 2 Interventional Active, not recruiting Acute Myeloid Leukemia, in Relapse
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

GO-203-2c is a cell-penetrating peptide that binds to MUC1, a protein that causes cancer (oncoprotein). MUC1 is over-expressed in many human cancers, such breast, prostate, lung, colon, pancreas, and ovary cancer, and has been associated with poor prognosis. GO-203-2c blocks homodimerization of the MUC1-C subunit required for nuclear translocation and downstream signaling. This binding eventually leads to cell death (in laboratory setting). Since MUC1 is over-expressed in many cancers, the potential of GO-203-2c in treatment of cancers is being investigated. A phase I clinical trial has been completed in which GO-203-2c was shown to be safe and demonstrating both anti-leukemia and immunomodulatory effects. A phase II study is investigating its potential in the treatment of Acute Myeloid Leukemia.
Status:
Investigational
Source:
INN:salnacedin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Salnacedin (also known as G 201) was developed as a topical anti-inflammatory agent; Salnacedin participated in phase II clinical trials in the USA for the treatment of dermatitis, acne, and psoriasis. However, all these studies were discontinued.
Status:
Investigational
Source:
NCT01327495: Phase 2/Phase 3 Interventional Completed Healthy
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Merrion Pharmaceuticals was developing an oral tablet formulation of acyline, a gonadotropin-releasing hormone (GnRH) antagonist, referred to as MER 104. MER-104 effectively suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion in man. Acyline has been investigated for the prevention and treatment of hypogonadism and contraception. Injectable forms have been administered successfully in man in Phase II studies as part of a potential contraceptive regimen. MER-104 is an enteric coated acyline tablet developed by Merrion Pharmaceuticals using GIPET™ I technology to enable the oral administration of this decapeptide. The development of acyline appears to have been discontinued.
Status:
Investigational
Source:
INN:maitansine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Maytansine is an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata. Maytansine inhibits the assembly of microtubules by binding to tubulin at or near the vinblastine-binding site, decreases microtubule dynamic instability and cause mitotic arrest in cells. It exerts cytotoxicity against a number of tumor cell lines and inhibits tumor growth in vivo. However, in human clinical trials, maytansine showed a small therapeutic window due to its neurotoxicity and harmful effects on the gastrointestinal tract. The potent cell killing ability of maytansine can be used in a targeted delivery approach, such as an antibody-drug conjugate, for the selective delivery of the drug and destruction of cancer cells.
Status:
Investigational
Source:
INN:ladirubicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LADIRUBICIN is an idarubicin derivative with potential antineoplastic activity. Its primary effect is a DNA alkylation with sequence specificity similar to that of conventional nitrogen mustards. It possesses a wide spectrum antitumor activity against rapidly proliferating murine leukemias and on slowly growing transplantable human tumor xenografts.