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Restrict the search for
beta carotene
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Status:
Investigational
Source:
INN:naltalimide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Naltalimide (TRK-130), a mu opioid receptor partial agonist, is being developed by Toray Industries for the treatment of overactive bladder. A phase IIb trial is underway in Japan. In radioligand-binding assays with cells expressing human µ-opioid receptors (MORs), δ-opioid receptors (DORs), or κ-opioid receptors (KORs), TRK-130 showed high selectivity for MORs (Ki for MORs, DORs, and KORs = 0.268, 121, and 8.97 nM, respectively). TRK-130 is a potent and selective human MOR partial agonist without undesirable opioid adverse effects such as constipation and enhances the storage function by suppressing the afferent limb of the micturition reflex pathway.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oprozomib (PR-047) is an orally bioavailable derivative of carfilzomib, with similar biological activity, i.e. inhibition of the chymotrypsin-like activity of the proteasome. It inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Oprozomib (PR-047) is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase I/II trial ongoing.
Status:
Investigational
Source:
USAN:MAFODOTIN [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mafodotin (mc-MMAF) is a hydrophilic non-cleavable antimicrotubule and antimitotic agent, monomethyl auristatin F (MMAF) derivative, having a maleimidocaproyl linker (mc linker), which is ready to conjugate to an antibody or other proteins or biopolymers. Antibody-drug conjugates having mafodotin such as Depatuxizumab mafodotin and Belantamab mafodotin have undergone clinical trials for the treatment of neoplasms.
Status:
Investigational
Source:
INN:ilorasertib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ilorasertib (previously known as ABT-348), an orally bioavailable ATP-competitive inhibitor of Aurora kinases (A, B and C), as well as the VEGF and PDGF families of receptor tyrosine kinases, was developed by AbbVie as an antineoplastic agent. It is known that Aurora kinases A, B, and C play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. Both VEGFRs and PDGFRs may be upregulated in various tumor cell types. Ilorasertib alone or in combination with azacitidine demonstrated activity in preclinical models in various hematological malignancies, indicating that pan-Aurora kinase and multiple kinase inhibition may have preferential antileukemic activity. Ilorasertib participated in phase I clinical for patients with advanced hematologic malignancies. The result has shown that the drug could be further studied in acute myelogenous leukemia. Ilorasertib is also going to be studied in phase II clinical trials to learn if this drug can help to control CDKN2A-deficient cancer in patients with advanced cancers.
Status:
Investigational
Source:
INN:flutafuranol (¹⁸F) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Flutafuranol F-18 (also known as NAV4694), a fluorine-18 labeled positron emission tomography (PET) imaging agent that was developed for diagnostic use. Flutafuranol F-18 binds to beta-amyloid deposits in the brain that could then be imaged in PET scans. It is known that amyloid plaque pathology is a required feature of Alzheimer’s disease (AD) and the presence of amyloid pathology is a supportive feature for the diagnosis of probable AD. Patients who are negative for amyloid pathology do not have AD. Thus, flutafuranol F-18 was studied in phase III clinical trial as an aid in the imaging for patients with Alzheimer’s disease and in phase II clinical trial for patients with mild cognitive impairment.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Defactinib is an oral, investigational drug candidate for the treatment of various solid tumors. Through dual inhibition of FAK and PYK2, defactinib targets key resistance mechanisms in the tumor microenvironment (TME), including limited local immune response, dense stroma, and resident cancer stem cells, that may limit the effectiveness of current and investigational treatments. Treatment-related adverse events are: unconjugated hyperbilirubinemia, fatigue and headache.
Status:
Investigational
Source:
NCT00716794: Phase 1/Phase 2 Interventional Completed Prostate Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235, Apoptone) is an orally bioavailable synthetic analogue of 3β-androstanediol, that is active in rodent models of prostate and breast cancer. HE3235 is a second generation antitumor agent that causes apoptosis. It is an androgen receptor antagonist. HE3235 inhibits the BCL2 gene which translates proteins that prevent apoptosis and stimulates the expression proteins that induce apoptosis. HE3235 also downregulates the gene that codes for the multi-drug resistant protein ABCG2 (BCRP1 – Breast Cancer Resistance Protein1). Apoptone was in Phase I/II trials to treat hormone-refractory prostate cancer. However, the development has been discontinued.
Status:
Investigational
Source:
NCT02294266: Phase 1 Interventional Completed Amphetamine-Related Disorders
(2014)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.
Status:
Investigational
Source:
J Int Soc Sports Nutr. Feb 2021;18(1):15.: Not Applicable Human clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
Clin Pharmacol Ther. May 2021;109(5):1274-1281.: Not Applicable Human clinical trial Completed Multiple System Atrophy/blood
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
