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

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Showing 421 - 430 of 528 results

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:ORBOFIBAN ACETATE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:roxifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Roxifiban (also known as DMP754), a potent antiplatelet agent in inhibiting platelet aggregation, and has a high specificity and affinity for human platelet glycoprotein IIb/IIIa complex (GPIIb/IIIa) receptors. Roxifiban participated in clinical trials phase III for the treatment of peripheral arterial disorders. This drug was also well tolerated in patients with chronic stable angina pectoris and was studied in the treatment of heparin-induced thrombocytopenia, and thrombosis. However, the development of this drug appears to have been discontinued.
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:
INN:delmadinone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Delmadinone is a steroid with progestogenic, anti-androgenic and weak glucocorticoid action, synthesized in Syntex S.A. Acetate ester of delmadinone is used in veterinary under tradenames Tardak for cats and dogs for the treatment of excessive or aberrant sexual behaviour, including vagrancy, for the relief of prostatic hypertrophy, circum-anal tumors and for the treatment of certain forms of aggressiveness, nervousness, epileptiform seizures and corticosteroid-resistant pruritus. Delmadinone acetate blocks androgen receptors inhibit 5-reductase, which catalyzes the transformation of testosterone to the more potent androgen 5-dihydrotestosterone and decreases the production of testosterone by inhibiting gonadotropin release.
Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.
Status:
Investigational
Source:
INN:trestolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.
Status:
Investigational
Source:
INN:ametantrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.
Status:
Investigational
Source:
INN:quindecamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Quindecamine (also known as UCL-1407) is quinaldine derivative with antibiotic and fungicidal activity. Treatment of rats and mice with Quindecamine (250 mg/kg/ day) each day for 4 weeks followed by 500 mg/kg/day for 2 more weeks reduced spontaneous motility and body weight but produced no pathological abnormalities of the various organs studied. In vitro, the drug showed very good activity against Staphylococcus aureus, Streptococcus hemolyticus, Candida albicans, Trichophyton mentagrophytes, and T. vaginalis. The drug had very good activity in 180 human subjects with various bacterial and mycotic diseases of the skin and mucosa when applied as a 1% salve.
Status:
Investigational
Source:
INN:stenbolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Stenbolone is an anabolic–androgenic steroid of the dihydrotestosterone group patented by Schering AG but never marketed. Ester prodrug of stenbolone is used as an anabolic–androgenic steroid for depot intramuscular injection under the brand names Anatrofin and Stenobolone.

Showing 421 - 430 of 528 results