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Restrict the search for
amphotericin b
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
ISATORIBINE, a guanosine analog, is an immunopotentiating agent. It is a selective agonist of toll‐like receptor 7, a pattern-recognition receptor that activates the innate immune response.
Status:
Investigational
Source:
NCT00659802: Phase 2 Interventional Completed Ulcerative Colitis
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Andrographolide, a diterpenoid, is known for its anti-inflammatory effects. It can be isolated from various plants of the genus Andrographis, commonly known as 'creat'. Andrographolide has been tested for its anti-inflammatory effects in various stressful conditions, such as ischemia, pyrogenesis, arthritis, hepatic or neural toxicity, carcinoma, and oxidative stress. Apart from its anti-inflammatory effects, andrographolide also exhibits immunomodulatory effects by effectively enhancing cytotoxic T cells, natural killer (NK) cells, phagocytosis, and antibody-dependent cell-mediated cytotoxicity (ADCC). The properties of andrographolide, such as its ability to induce apoptosis of cancer cells and inhibition of DTH, its anti-oxidative and cytoprotective effect, and its ability to enhance CTLs and NK cell activation makes it a potent antiviral agent. Andrographolide inhibited the growth of human breast, prostate, and hepatoma tumors. Andrographolide could be a potent anticancer agent when used in combination with other chemotherapeutic agents.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifamides (NSC-143418) are drugs used in the treatment of tuberculosis. They also have immunosuppressive activity, the exact mechanism of which is still unknown, although the ability of rifamides to inhibit tumor necrosis factor (TNF)-induced NF-kB activation may be associated with it. A variety of rifamide analogues exist, such as rifamycin B, rifapentine, rifamycin SV, rifabutin and rifampicin.
Class (Stereo):
CHEMICAL (RACEMIC)
Tropirine is an antihistaminic, respiratory, anticholinergic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Lurosetron (GR 87442) is a serotonin 5HT3 receptor antagonist. It was undergoing clinical evaluation with Glaxo Wellcome in the UK as a potential drug for the treatment of emesis.
Class (Stereo):
CHEMICAL (UNKNOWN)
Tolafentrine is phosphodiesterase 3/4 (PDE3/4) inhibitor. Treatment of endothelial cells with tolafentrine significantly decreased asymmetrical dimethylarginine-induced apoptosis via a cAMP/PKA-dependent pathway by induction of dimethylarginine dimethylaminohydrolase 2 (DDAH2). Chronic nebulization of PDE3/4 inhibitor significantly attenuated monocrotaline-induced hemodynamic, gas exchange abnormalities, vascular remodeling, and right heart hypertrophy. When chronically nebulized from day 28 to 42 (12 daily aerosol maneuvers), after full establishment of severe pulmonary hypertension, tolafentrine reversed about 60% of all hemodynamic abnormalities in rats, right heart hypertrophy and monocrotaline-induced structural lung vascular changes, including the proportion of pulmonary artery muscularization. Tolafentrine was developed as therapeutic agent for the treatment of asthma. However, this development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Valtrate is a principle compound isolated from Valeriana jatamansi Jones, which is a Traditional Chinese Medicine used to treat various mood disorders. Valtrate at a high dose has been found to have sedative properties by inhibiting spontaneous motion and increasing the sleeping number induced by pentobarbital sodium in mice. In rats valtrate exhibits anxiolytic-like profiles in the elevated plus maze test and the open field test. Valtrate attenuated HPA axis activity by reducing the corticosterone level. Valtrate also possesses anti-breast cancer activities via cell cycle arrest, apoptosis, and inhibition of cell migration, thus supporting valtrate as a potential antitumor agent.
Status:
Investigational
Source:
NCT00529659: Phase 2 Interventional Completed Sarcopenia
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
MK-0773 is an orally active selective androgen receptor modulator. The safety and efficacy of MK-0773 was evaluated in sarcopenic elderly women. The MK-0773- induced improvements in lean body mass were not accompanied by statistically significant improvements in physical function. Higher dose of MK-0773 or longer duration of therapy might have resulted in improvements in physical function, but liver transaminase elevations likely preclude further development of MK-0773. Drug-candidate had been in phase I clinical trials for the treatment of osteoporosis.
Status:
Investigational
Source:
NCT00003021: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(1997)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bizelesin (previously known as U-77779 or NSC 615291), a cyclopropylpyrroloindole antitumor agent acts as a bifunctional alkylating agent and produces DNA interstrand cross-links. This drug participated in phase I clinical trials in patients with advanced solid malignancies, however further development was discontinued.
Status:
Investigational
Source:
NCT00952588: Phase 2/Phase 3 Interventional Completed Acute Myeloid Leukemia
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Barasertib (AZD1152) is a dihydrogen phosphate prodrug of a pyrazoloquinazoline Aurora kinase inhibitor [AZD1152–hydroxyquinazoline pyrazol anilide (HQPA)] and is converted rapidly to the active AZD1152-HQPA in plasma. AstraZeneca was developing the aurora kinase inhibitor, barasertib (AZD 1152) as a therapeutic for cancer. AZD1152-HQPA is a highly potent and selective inhibitor of Aurora B (Ki, 0.36nmol/L) compared with Aurora A (Ki, 1,369nmol/L) and has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumour cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis. Barasertib (AZD1152) potently inhibited the growth of human colon, lung, and haematologic tumour xenografts (mean tumour growth inhibition range, 55% to ≥100%; P < 0.05) in immunodeficient mice. Detailed pharmacodynamic analysis in colorectal SW620 tumour-bearing athymic rats treated i.v. with Barasertib (AZD1152) revealed a temporal sequence of phenotypic events in tumours: transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells (>4N DNA, 2.3-fold higher compared with controls). Histologic analysis showed aberrant cell division that was concurrent with an increase in apoptosis in AZD1152-treated tumours. Bone marrow analyses revealed transient myelosuppression with the drug that was fully reversible following cessation of Barasertib (AZD1152) treatment. Barasertib (AZD1152) was in phase III for the treatment of Acute myeloid leukaemia, but later these studies were discontinued.
