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Restrict the search for
vitamin a
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Class (Stereo):
CHEMICAL (ACHIRAL)
Cianopramine is a highly potent inhibitor of neuronal serotonin (5-HT) uptake developed by Hoffmann-La Roche for major depression treatment. In preclinical studies, acute and chronic treatment with Cianopramine shows clear behavioural effects Cianopramine increases neophobic reactions in the free exploration test, the avoidance reaction to a brightly illuminated chamber in the light/dark choice procedure as well as to open arms in the elevated plus-maze test. In a double-blind trial, Cianopramine effective in reducing scores on the Hamilton Psychiatric Rating Scale for Depression and on a global scale. Unfortunately, Cianopramine administrations were associated with significant adverse effects and future development was discontinued.
Status:
Investigational
Source:
NCT01817959: Phase 3 Interventional Completed Islet Transplantation in Diabetes Mellitus Type 1
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Reparixin is a CXC chemokine receptor type 1 (CXCR1) and type 2 (CXCR2) inhibitor. This compound has potential antineoplastic activity. It can be administered orally, binds to CXCR1 (overexpressed on cancer stem cells) and prevents its activation by its ligand interleukin 8. This might result in the death of cancer cells and inhibition of cell progression and metastasis. Reparixin also inhibits CXCR2 activation, possibly reducing both neutrophil recruitment and vascular permeability during inflammation or injury. A phase II clinical trial evaluating the effects of orally administered reparixin on cancer stem cells in the primary tumor and the tumoral microenvironment in an early breast cancer population was terminated. Reparixin has also been suggested as a novel potential therapeutic strategy for aggressive forms of thyroid cancer, based on results of a xenotransplantation study in mice.
Status:
Investigational
Source:
NCT00068952: Phase 3 Interventional Completed Glioblastoma
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Edotecarin (J-107088 or [6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carb azo le-5,7(6H)-dione]) is a DNA topoisomerase I inhibitor. The antitumor activity of edotecarin has been tested in vitro and in vivo, and inhibition of tumor growth has been observed in breast, cervix, pharynx, lung, prostate, colon, gastric, and hepatic cancer models. Banyu Pharmaceutical Co Ltd and Pfizer Inc were developing edotecarin for the potential treatment of solid tumors. Edotecarin development has been discontinued.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Methoxyphedrine (para-methoxymethcathinone, 4-methoxymethcathinone, bk-PMMA, PMMC, Methedrone, 4-MeOMC) is a phenethylamine, amphetamine, and cathinone derivative that acts as a triple reuptake/release/reversible monoamine oxidase inhibitor and used as a recreational drug. Methedrone has been found to be a potent serotonin transporter (SERT) and norepinephrine transporter (NET) inhibitor, but a weak dopamine transporter (DAT) inhibitor. Methedrone induces the transportation mediated release of NE, DA, and 5-HT from cells preloaded with monoamines making it a serotonin-norepinephrine-dopamine (SNDRA) releasing agent, also known as triple releasing agent (TRA), which is a common characteristic among drugs of abuse. The health risks associated with Methedrone are unknown but are expected to be similar to other cathinones. The deaths of two young men in southeast Sweden in 2009 were attributed to Methedrone overdose.
Status:
Investigational
Source:
NCT00831103: Phase 2 Interventional Completed Herpes Zoster
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Omaciclovir (previously known as H2G), a cyclic guanosine analog that is structurally similar to acyclovir and was in clinical development for the treatment of herpesvirus infections. This drug acted against varicella-zoster virus (VZV), by the formation of high concentrations of relatively stable H2G-triphosphate, which is a potent inhibitor of the viral DNA polymerases. However, further development of this drug was discontinued.
Status:
Investigational
Source:
NCT01594723: Phase 2 Interventional Active, not recruiting Neoplasms, Hematologic
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. Gandotinib is in phase II clinical trials by Lilly for the treatment of myeloproliferative disorders.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Palosuran, also known as ACT-058362, a potent and specific antagonist of
the human UT receptor. Urotensin inhibition with palosuran was a promising alternative in pulmonary arterial hypertension. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Palosuran improves pancreatic and renal function in diabetic rats. Phase-II clinical trials for diabetic nephropathies and cardiovascular disorders were discontinued.
Status:
Investigational
Source:
NCT00006363: Phase 3 Interventional Completed Adult Acute Basophilic Leukemia
(2000)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Valspodar (PSC-833) is a derivative of cyclosporin but devoid of the immunosuppressive and nephrotoxic properties seen in cyclosporin A. It exhibited high-affinity binding to Mdr1 P-glycoprotein (P-gp) and demonstrated multidrug resistance-reversing activity superior to cyclosporin A and verapamil both in vitro and in vivo. Preclinical and phase I/II clinical data have indicated that plasma levels of PSC-833 with multidrug resistance-reversing activities are achievable. Potent inhibition of intestinal, hepatobiliary and blood-brain barrier P-gp function has been demonstrated. The toxicity profiles of valspodar are acceptable and dose-limited by transient and reversible cerebellar ataxia. It has shown multidrug resistance-modulating activities towards acute myeloid leukemia, multiple myeloma and ovarian cancer in phase I/II clinical trials. However, the company discontinued development of valspodar in April 2001 following disappointing results reported from several multicentre phase III studies.
Status:
Investigational
Source:
NCT00709865: Phase 3 Interventional Completed Renal Insufficiency
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tonapofylline is a selective oral adenosine A, receptor antagonist, for the potential treatment of congestive heart failure. Oral tonapofylline over the dose range of 3 to 225 mg/day produced significant increases in sodium excretion in patients with stable heart failure without causing kaliuresis or reducing renal function. Tonapofylline may be useful in the clinical setting for the prevention of kidney failure induced by nephrotoxic agents such as cisplatin. Tonapofylline may be renoprotective in the setting of concomitant treatment with a loop-diuretic. Adverse effects were generally mild. Tonapofylline had been in phase III clinical trial for the treatment of acute heart failure. However, this development was discontinued.
Status:
Investigational
Source:
INN:indatraline [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Indatraline (Lu 19-005) is a non-selective monoamine transporter inhibitor that has been shown to block the reuptake of dopamine, norepinephrine, and serotonin with effects similar to those of cocaine. In vivo, indatraline produced behavioral effects suggestive of enhanced dopaminergic, noradrenergic, and serotonergic activity in mice. Indatraline also substituted for a high dose of cocaine in rats trained to discriminate between a low and a high dose of cocaine, which demonstrates that indatraline produces cocaine-like discriminative stimulus effects. Indatraline has been studied to block the action of methamphetamine and MDMA.
