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

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Showing 71 - 80 of 1904 results

Status:
Investigational
Source:
INN:timobesone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Timobesone is a topical corticosteroid and thiol ester derivative with anti-inflammatory activity.
Status:
Investigational
Source:
USAN:CUPRIC ACETATE CU 64 [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cu-64 is a radioisotope of copper with T1/2 12.7 hours. It decays by emission of beta+ particles with energies 0.653 (17.8%) MeV, which makes it suitable for positron emission tomography. The most widely used Cu chelators are DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid). Cu-64 acetate is used as a model compound to study metabolism and distribution of Cu-64.
Status:
Investigational
Source:
INN:laurolinium acetate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAUROLINIUM, a quaternary ammonium compound, is a cationic antimicrobial agent. It has a broad spectrum of activity against Gram‐positive and Gram‐negative bacteria, fungi, and protozoan Trichomonas vaginalis. It is suitable for use in the treatment of local infections, for the sterilization of skin areas and for general antiseptic purposes.
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.
Status:
Investigational
Source:
NCT01128335: Phase 2 Interventional Completed Liver Transplantation
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound that potently inhibits the PKC α, β and the θ isoforms resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.
Status:
Investigational
Source:
Acta Endocrinol (Copenh). 1966;53:Suppl 111:3-26.: Not Applicable Human clinical trial Completed Menstruation Disturbances
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Pregnanediol is a chief steroid metabolite of progesterone that is biologically inactive and occurs as pregnanediol glucuronate in the urine. Pregnanediol has two hydroxyl groups, at 3-alpha and 20-alpha. A test can be done to measure the amount of pregnanediol in urine. The urine test offers an indirect way to measure progesterone levels in the body. It is a standard in the colorimetric determination of urinary pregnanediol in clinical laboratories.
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:
NCT00002462: Phase 3 Interventional Active, not recruiting Lymphoma
(1989)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01009931: Phase 2 Interventional Terminated Leukemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phorbol 12-myristate 13-acetate (PMA) also commonly known as 12-O-Tetradecanoylphorbol-13-acetate (TPA) is a phorbol ester that is commonly used to activate phospholipid-dependent protein kinase (protein kinase C). PMA/ TPA possesses potential antineoplastic effects and was studied in phase II clinical trials together with dexamethasone in patients with relapsed or refractory acute myeloid leukemia. In addition, PMA/ TPA participated in phase I trial for treating patients with hematologic cancer or bone marrow disorder that has not responded to previous treatment. Nevertheless, both clinical trials were terminated. Besides, PMA/ TPA was studied in patients with solid tumors, which had depressed white blood cell and neutrophil counts because of prior treatment with cytotoxic cancer chemotherapeutic drugs. It was shown, that the drug increased the low white blood cell and neutrophil counts toward the normal range.
Status:
Investigational
Source:
NCT00003241: Phase 2 Interventional Completed Brain and Central Nervous System Tumors
(1998)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phenylacetate is the ester of a phenol and acetic acid. It is a metabolite of anticancer drug phenylbutyrate (PB), natural neurotransmitter phenylethylamine. Naturally, it is an odorant found in strawberries, passion fruit, and black tea. Phenylacetate level in urine was used as a marker for the diagnosis of some forms of unipolar major depressive disorders. Phenylacetate is used as a tool substrate to study esterase activity in the blood of patients in clinical studies of the effect of nutritional supplements on paraoxonase-1 levels.