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Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Bentiamine (also known as dibenzoyl thiamine), a derivative of thiamine, is rapidly absorbed and converted to thiamine. Experiments on rodent have shown that this compound had low toxicity and absence of carcinogenicity.
Status:
Investigational
Source:
NCT01320579: Phase 2 Interventional Completed Atopic Dermatitis
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Urocanic acid is a breakdown (deamination) product of histidine. In the liver, urocanic acid is an intermediate in the conversion of histidine to glutamic acid, whereas in the epidermis, it accumulates and may be both a UV protectant and an immunoregulator. Urocanic acid (UA) exists as a trans isomer (t-UA, approximately 30 mg/cm2) in the uppermost layer of the skin (stratum corneum). t-UA is formed as the cells of the second layer of skin become metabolically inactive. During this process, proteins and membranes degrade, histidine is released, and histidase (histidine ammonia lyase) catalyzes the deamination of histidine to form t-UA. t-UA accumulates in the epidermis until removal by either the monthly skin renewal cycle or sweat. Upon absorption of UV light, the naturally occurring t-UA isomerizes to its cis form, c-UA. Because DNA lesions (e. g. , pyrimidine dimers) in the lower epidermis can result from UV-B absorption, initial research proposed that t-UA acted as a natural sunscreen absorbing UV-B in the stratum corneum before the damaging rays could penetrate into lower epidermal zones. c-UA also suppresses contact hypersensitivity and delayed hypersensitivity, reduces the Langerhans cell count in the epidermis, prolongs skin-graft survival time, and affects natural killer cell activity. It has also been proposed that c-UA may mediate the transient alteration in immune surveillance resulting in immunosuppression induced after UV-irradiation, by interacting with immune cells locally and/or systemically to generate T cells with suppressor function.
Status:
Investigational
Source:
NCT01712061: Phase 2 Interventional Completed Diabetic Nephropathy
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
PF-04634817 is a small molecule chemokine CCR2 and CCR5 receptor dual antagonist. Treatment with PF-04634817 was associated with a modest improvement in best-corrected visual acuity, which was inferior to intravitreal ranibizumab. Analysis of the primary endpoint, Urine Albumin-to-Creatinine Ratio, indicated a modest effect of PF-04634817 in reducing albuminuria in subjects with type 2 diabetes who received angiotensin receptor blocker therapy after 12 weeks of treatment. Despite the tolerable safety profile shown by PF-04634817, clinical development was discontinued in light of the modest efficacy observed.
Status:
Investigational
Source:
NCT03703310: Phase 3 Interventional Completed Basal Cell Nevus Syndrome
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
FIN-6 (PATIDEGIB, IPI-926), a semisynthetic derivative of alkaloid cyclopamine, is a G protein-coupled receptor Smoothened (Smo) inhibitor with antineoplastic activity. Smo is a key signaling transmembrane protein in the Hedgehog signaling pathway which plays an important role in the proliferation of neuronal precursor cells in the developing cerebellum and other tissues. FIN-6 (PATIDEGIB, IPI-926) is under development for Gorlin syndrome, basal cell carcinomas, and other potential indications.
Status:
Investigational
Source:
NCT01039701: Phase 2 Interventional Completed Mild to Moderate Alzheimer's Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Status:
Investigational
Source:
NCT04251182: Phase 2 Interventional Completed Alzheimer Disease
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:triclofenol piperazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
2,4,5-Trichlorophenol is a grey flake or needle-shaped solid. It is used as an intermediate in the manufacture of the herbicide 2,4,5-Trichlorophenoxyacetic Acid (2,4,5-T) and as a fungicide and bactericide. 2,4,5-trichlorophenol (triclofenol piperazine, Ranestol) is an antifungal agent, which was also used against light hookworm infections. Thirty persons who were positive for hookworm eggs in their stools were treated with 50 mg/kg of triclofenol piperazine dissolved in 5 per cent polyethylene glycol Ranestol® in soft gelatin capsules. Nineteen of these showed 77 to 100 % reduction in egg count average when compared with the pre-treatment counts. Side reactions were limited to mild and transient nausea in 23, vomiting in 7, transient abdominal cramps and headache in 2 each. 2,4,5-trichlorophenol complexed with dicyclohexylamine was used for treatment of experimental mycosis. From the mycological and clinical evaluation the conclusion can be drawn that the effect of phenol in lipophilic ointment is comparable to that of clotrimazole.
Status:
Investigational
Source:
NCT01291108: Phase 2 Interventional Completed Glaucoma, Open-Angle
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Simenepag (AGN-210676) is a a small molecule selective prostaglandin EP2 agonist with EC50 of 5 nM. Allergan was developing simenepag for the treatment of glaucoma and ocular hypertension.
Status:
Investigational
Source:
NCT01924403: Not Applicable Interventional Completed Total Knee Arthroplasty
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrithiobac sodium (also known as PE350) is a carboxyphenylthiodimethoxypyrimidine derivative patented by Kumiai Chemical Industry Co., Ltd. and Ihara Chemical Industry Co., Ltd. as herbicide and commercialized for uses in cotton cultivation. Pyrithiobac acts as a potent inhibitor of Acetohydroxyacid synthase (AHAS), also known as acetolactate synthase, that catalyzes the first reaction in the pathway for synthesis of the branched-chain amino acids. Pyrithiobac is applied POST at 70 g/ha in cotton (1- to 2-leaf stage) for effective control of several broadleaf weeds such as Xatithium stmmarium, Ipomoea spp., Abutilon theophrasli, Sesbania exaltata (hemp sesbania), Salvia reflexa, Sida spinosa, Amaranthus spp., etc. When applied at this rate, wheat, soybean and grain sorghum may be rotated with cotton with no crop toxicity to these crops. Cotton is very tolerant of Pyrithiobac even at rates as high as 112 g/ha. It may also be applied PPI or PRE in cotton to control Cassia occidentalis, a troublesome broadleaf weed. Higher rates cause injury to cotton. However, caution may need to be exercised, as insecticides (malathion, fenvalerate, methomyl, chlorpyriphos, etc.) applied along with Pyrithiobac, as mixtures are likely to make cotton sensitive to the herbicide.
Status:
Investigational
Source:
NCT01975610: Phase 2 Interventional Completed Rheumatoid Arthritis
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Spebrutinib (CC-292, AVL-292) is a selective inhibitor of BTK that was under clinical development for the treatment of rheumatoid arthritis (phase II) and B-cell Lymphoma (phase I). The drug was discovered by Avila Therapeutics, but then acquired by Celgene. Spebrutinib covalently binds to Cys 481 in BTK, blocking the ATP-binding pocket of the enzyme. The drug is no longer in Celgene's pipeline and its development is supposed to be terminated.