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Showing 1691 - 1700 of 24423 results

Fonturacetam, also known as Phenylpiracetam, is marketed in Russia as Carphedon and Phenotropil. It is one of the first ever nootropic drugs and originally discovered in Russia. Fonturacetam acts on most neurotransmitter systems and has been used for its cognitive and physical enhancing properties, and also as an antidepressant.
Status:
Investigational
Source:
NCT02152982: Phase 2/Phase 3 Interventional Active, not recruiting Glioblastoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Veliparib (ABT-888) is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models. AbbVie is developing veliparib for the treatment of cancers. Clinical trials are underway worldwide, investigating veliparib primarily as part of a combination therapy in oncology indications such as brain, colorectal, melanoma, ovarian, prostate and pancreatic cancers.
Status:
Investigational
Source:
INN:lirequinil
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lirequinil is a benzoquinolizinone derivative. It is a partial agonist to the benzodiazepine (BDZ) receptor. Lirequinil slightly lowered the rhythmic slow-wave activity frequency during waking mobility. Lirequinil acts more selectively than nitrazepam to promote the drowsy EEG pattern, and the partial agonistic properties may minimize the residual effects during waking mobility similar to the short-acting agent zopiclone. Lirequinil was well tolerated at all doses, causing no clinically relevant changes in vital signs or laboratory parameters. At doses of 10 and 30 mg there were signs of unsteady gait, indicating a central nervous system depressant effect. Lirequinil had been in phase II for the treatment of sleep disorders.
Status:
Investigational
Source:
NCT00394628: Phase 1/Phase 2 Interventional Unknown status Glioblastoma Multiforme
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Banoxantrone (formally known as AQ4N), a bioreductive drug that is irreversibly converted to AQ4, a stable DNA affinic cytotoxic compound. Banoxantrone is activated by haem-containing reductases such as inducible nitric oxide synthase (iNOS). In hypoxic cells, AQ4N is reduced to the topoisomerase II inhibitor AQ4. By inhibition of topoisomerase II within these hypoxic areas, AQ4N has been shown to sensitize tumors to existing chemo- and radiotherapy treatments. Novacea, the company which was responsible for clinical trials for banoxantrone had decided to scale back on its clinical development, including discontinuing the clinical trial in acute lymphoblastic leukemia and delaying the planned clinical trial in B-cell lymphoma. The company decided to continue enrollment in an ongoing Phase 1b/2a clinical trial in patients with glioblastoma multiforme. However, further information about these clinical trials are not available. Some recent experiments have shown that targeting hypoxic tumors with high levels of iNOS with a combination of AQ4N and radiotherapy could be a useful clinical therapeutic strategy.
Status:
Investigational
Source:
NCT00788333: Phase 1/Phase 2 Interventional Completed Breast Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



BMS-754807 is a small-molecule insulin-like growth factor 1 receptor (IGF-1R) antagonist that was being developed by Bristol-Myers Squibb. BMS-754807 is a potent and reversible inhibitor of the insulin-like growth factor 1 receptor/insulin receptor family kinases (Ki, <2 nmol/L). It is currently in phase II development for the treatment of a variety of human cancers. BMS-754807 effectively inhibits the growth of a broad range of human tumor types in vitro, including mesenchymal (Ewing's, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreatic, colon, gastric), and hematopoietic (multiple myeloma and leukemia) tumor cell lines (IC50, 5-365 nmol/L); the compound caused apoptosis in a human rhabdomyosarcoma cell line, Rh41, as shown by an accumulation of the sub-G1 fraction, as well as by an increase in poly ADP ribose polymerase and Caspase 3 cleavage. BMS-754807 is active in vivo in multiple (epithelial, mesenchymal, and hematopoietic) xenograft tumor models with tumor growth inhibition ranging from 53% to 115% and at a minimum effective dose of as low as 6.25 mg/kg dosed orally daily. Combination studies with BMS-754807 have been done on multiple human tumor cell types and showed in vitro synergies (combination index, <1.0) when combined with cytotoxic, hormonal, and targeted agents. The combination of cetuximab and BMS-754807 in vivo, at multiple dose levels, resulted in improved clinical outcome over single agent treatment. These data show that BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.
Status:
Investigational
Source:
INN:ilepatril [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ilepatril, previously known as AVE7688, an inhibitor of neutral endopeptidase and angiotensin-converting enzyme (ACE), was initially being developed for cardiac failure. Ilepatril was in phase IIb/III clinical trials for hypertension and in phase II trials for diabetic nephropathy, however, studies were discontinued.
Status:
Investigational
Source:
INN:megalomicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Megalomicin is a Micromonospora-produced macrolide antibiotic complex. Megalomicin A component was studied most extensively. It inhibited the ATP-dependent acidification of lysosomes and intra-Golgi transport in vitro. Megalomicin induces a powerful inhibitory effect on HIV-1 replication at nontoxic concentrations by preventing the processing of HIV-1 gp160 envelope protein and the subsequent formation of infectious viral particles.
Status:
Investigational
Source:
USAN:Abamectin Component B1a
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Avermectin B1a (AVM B1a), a widely used insecticide and acaricide, is reported to both activate and inhibit gamma-aminobutyric acidA (GABA(A)) receptor function in mammalian brain. Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis. AVM B1a binds to two different sites in the GABA-gated chloride channel with dual effects, i.e., activating the channel on binding to the high-affinity site and blocking it on further binding to the low-affinity site.
Status:
Investigational
Source:
NCT03672708: Not Applicable Interventional Completed Gastric Intestinal Metaplasia
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:devazepide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Devazepide (L-364718 or MK-329) is a nonpeptide antagonist for the peripheral (type-A) cholecystokinin (CCK) receptor, which has proved effective in blocking the actions of both exogenous and endogenous CCK in several species. It is an orally active antagonist of CCK-stimulated pancreaticobiliary output in man. Devazepide has been developing for the treatment of anxiety, cancer, neuropathic pain however development discontinued.

Showing 1691 - 1700 of 24423 results