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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
NCT02425241: Phase 1/Phase 2 Interventional Completed HIV
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
RO-638695 (also known as Miridesap, CPHPC and GSK-2315698) is an antineoplastic and a serum amyloid P component inhibitor. RO-638695 almost completely depletes circulating serum amyloid P component (SAP), but a small amount of SAP is left for recognition by subsequently administered therapeutic IgG anti-SAP antibodies. SAP is a blood protein that is the target of a novel immunotherapy approach. RO-638695 has therefore been evaluated in phase I and II clinical trials for its safety and potential in treatment of diseases like Alzheimer’s disease, HIV infection and other diseases with systemic amyloid deposition.
Status:
Investigational
Source:
NCT01054118: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Arena Pharmaceuticals was developing APD-597 (JNJ-38431055), a small molecule, an orally active agonist of the G-protein coupled receptor 119 (GPR119), for the treatment of Type 2 diabetes mellitus. JNJ-38431055 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long-lasting metabolites with the potential to accumulate in clinical studies. In humans, single-dose oral JNJ-38431055 increased postmeal plasma glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic peptide (GIP), and peptide YY (PYY) concentrations but did not significantly decrease glucose excursion or increase insulin secretion. However, in a graded glucose infusion study, JNJ-38431055 was shown to induce a higher insulin secretion rate (ISR) relative to placebo at elevated plasma glucose levels. These studies provide evidence for the potential efficacy of JNJ-38431055 as an antidiabetes agent in humans.
Status:
Investigational
Source:
NCT03193853: Phase 2 Interventional Completed Triple Negative Breast Cancer
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Serabelisib (INK1117 and TAK-117) is an orally bioavailable, PI3K p110α- isoform-specific inhibitor with an in vitro IC50 of 15 nM, highly selective against other isoforms (p110β, p110γ, and p110δ) and mTOR (no significant inhibitions at 1 μM concentration). It displayed significant efficacy in several PI3Kα mutant-specific preclinical mouse xenograft tumor models, and blocked signaling to Akt and inhibited the growth of cancer cells harboring wild-type or mutated p110α. Preclinical studies showed TAK-117 to have the low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. Serabelisib is currently under clinical evaluation.
Status:
Investigational
Source:
NCT02091219: Not Applicable Human clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Targets:
Conditions:
24-Hydroxycalcidiol (24,25-dihydroxy vitamin D3) is a circulating metabolite of vitamin D3. 24,25(OH)2D3 functions by activation of Vitamin D receprtor and promotion of ostecalcin expression, but is less effective than other D3 metabolite, 1alpha,25(OH)2D3. There is conflicting evidence on efffect of 24-hydroxycalcidiol on bone metabolism. In several animal studies it was demonstrated that 24-hydroxycalcidiol was able to stimulate calcification of bone and restore the reduction in bone mineral apposition rate. However, no beneficial effect of 24R,25(OH)2D3 treatment of postmenapausal women on bone mineral density or bone loss and calcium metabolism were observed.
Status:
Investigational
Source:
INN:tracazolate [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tracazolate (ICI 136,753), a pyrazolopyridine, is a non-benzodiazepine with anxiolytic-like activity in animal models. It is known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. Its intrinsic efficacy, potentiation, or inhibition is determined by the nature of the third subunit (gamma1-3, delta, or epsilon) within the GABA(A) receptor complex.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tipredane is one of the compounds of a new series of sulfur-containing steroids synthesized at The Squibb Institute for Medical Research and is being developed for topical treatment of human dermatoses. Tipredane is structurally unique in that the classical l7-beta two-carbon side chain and the 17-alpha hydrogen of the steroid have been replaced by two alkylthio substituents. Tipredane has been shown to possess moderate to potent anti-inflammatory activity in various animal models, and to exhibit favorable separation of local anti-inflammatory activity from adverse systemic effects in both animals and humans. After oral administration, [3H]tipredane was rapidly absorbed, metabolized, and excreted into urine and feces. Metabolism of tipredane was rapid and complex, with significant species differences, although the disposition in rhesus and cynomolgus monkeys seemed to be similar to humans. Tipredane had been investigated as the therapeutic agent for the treatment of allergic rhinitis, asthma and skin disorders. However, this development was discontinued.
Status:
Investigational
Source:
NCT00579384: Phase 2 Interventional Completed Photosensitive Epilepsy
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Malethamer is the generic name of a new synthetic hydrocarbon copolymer with extraordinary water-binding properties, being able to absorb 200 times its weight of water. It is physically and chemically binds poliovirus 1 and certain bacterial enterotoxins. Ethylene-maleic anhydride copolymers and their derivatives have come to be considered for a number of applications generally involving the formation of insoluble complexes with proteins and viruses. The copolymer is not absorbed from the gastrointestinal tract and is pharmacologically inert. Malethamer, because of its water absorbing quality, is an effective compound for the symptomatic control of diarrhea, both organic and functional.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lexithromycin is an early semi-synthetic erythromycin, prepared by reaction of the 9-keto moiety to methyl oxime. Lexithromycin has improved absorption in vivo over erythromycin due to increased hydrophopicity and pH stability. Like all erythromycins, lexithromycin shows broad spectrum antibacterial activity and acts by binding to the 30S and 50S ribosomal sub-units, blocking protein synthesis. Formulations containing lexithromycin were tested in clinical trials as treatment for HIV but were discontinued.
Status:
Investigational
Source:
NCT00858377: Phase 1 Interventional Completed Advanced Malignancy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Amgen is developing AMG-900, an orally active, small molecule aurora kinase A, B and C inhibitor for the treatment of solid tumours and haematological malignancies. In tumor cells, AMG-900 inhibited autophosphorylation of aurora-A and -B as well as phosphorylation of histone H3 on Ser(10), a proximal substrate of aurora-B. The predominant cellular response of tumor cells to AMG-900 treatment was aborted cell division without a prolonged mitotic arrest, which ultimately resulted in cell death. AMG-900 inhibited the proliferation of 26 tumor cell lines, including cell lines resistant to the antimitotic drug paclitaxel and to other aurora kinase inhibitors (AZD1152, MK-0457, and PHA-739358), at low nanomolar concentrations. Furthermore, AMG-900 was active in an AZD1152-resistant HCT116 variant cell line that harbors an aurora-B mutation (W221L). Oral administration of AMG-900 blocked the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibited the growth of HCT116 tumor xenografts. Importantly, AMG-900 was broadly active in multiple xenograft models, including 3 multidrug-resistant xenograft models, representing 5 tumor types. AMG-900 has entered clinical evaluation in adult patients with advanced cancers and has the potential to treat tumors refractory to anticancer drugs such as the taxanes.
