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

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Showing 51 - 60 of 1357 results

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:
JAN:PREGNANDIOL [JAN]
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:
INN:dexbudesonide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dexbudesonide (22R- Budesonide) is an epimer R of Budesonide, last is used as a mixture of 22R and 22S epimers for the topical treatment of asthma, rhinitis, and inflammatory bowel disease
Status:
Investigational
Source:
Diabetes Obes Metab. Mar 2023;25(3):832-843.: Phase 2 Human clinical trial Completed Diabetes Mellitus, Type 2/complications
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Designated
Source:
FDA ORPHAN DRUG:640318
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)