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Restrict the search for
methylene blue
to a specific field?
Status:
Investigational
Source:
NCT02756130: Phase 1/Phase 2 Interventional Withdrawn High Grade Fallopian Tube Serous Adenocarcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Birinapant is a parenterally administered bivalent peptidomimetic of the SMAC protein (Second Mitochondria-derived Activator of Caspases) and is therefore known as a SMAC mimetic compound. Birinapant is a particularly potent antagonist of two members of the Inhibitor of Apoptosis Proteins (IAP) family, cIAP-1, and cIAP-2. cIAP-1 and -2 are ubiquitin ligases whose expression can protect cells from apoptosis and cause pro-survival effects of TNF-α and related ligands. When Birinapant binds to cIAP-1 or -2 it causes the protein to ubiquitinate itself, which in turn drives the degradation of the protein. In this way, birinapant suppresses the levels of cIAP-1 and cIAP-2 and therefore switches cell signaling to drive tumor cell apoptosis in the presence of TNF-α. Birinapant has been shown to give rise to sustained and substantial reductions of cIAP1 levels in Peripheral Blood Mononuclear Cells (PBMCs) and tumor tissue. To date, Birinapant has been dosed in approximately 450 patients across 9 studies. The majority of studies was in oncology (one in HBV) and primarily recruited patients with refractory solid tumors & hematological malignancies (dominated by ovarian, colorectal, acute myeloid leukemia and Myelodysplastic syndromes). Overall Birinapant has shown acceptable safety and tolerability for further development in oncology indications. The current plans are to study Birinapant clinically in combination with Keytruda® for the treatment solid tumors and in an Investigator-Initiated study at UCLA for high-grade serous carcinoma (HGSC) in combination with platinum-based chemotherapy.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Azaspirium was studied as a spasmolytic and antihypertensive agent.
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)
Etamocycline is a broad-spectrum antibiotic. It was studied in the treatment of bronchopulmonary and gastrointestinal infectious diseases.
Status:
Investigational
Source:
NCT00427856: Phase 2 Interventional Completed Lymphoma, Follicular
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl-
2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC).
The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.
Status:
Investigational
Source:
NCT01757860: Phase 1 Interventional Completed Drug Safety
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
1α-HYDROXYVITAMIN D5 (CARD-024) is non-hypercalcemic, selective vitamin D receptor agonist under development for the treatment of cardiovascular disease, secondary hyperparathyroidism in chronic kidney disease and intestinal bowel disease fibrosis. CARD-024 attenuated the pro-fibrotic response of colonic myofibroblasts to high matrix stiffness, suggesting that it may ameliorate intestinal fibrosis.
Status:
Investigational
Source:
NCT00909688: Phase 1 Interventional Completed Healthy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
BLI 489 was developed by Wyeth as a 6-methylidene-penem β-lactamase inhibitor for the treatment of bacterial infections and urinary tract infections. BLI-489 has shown the promising clinical data, however, development of this drug, was discontinued.
Status:
Investigational
Source:
INN:darbufelone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Darbufelone mesylate is a dual inhibitor of cellular prostaglandin and leukotriene production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 uM) but is much less potent with PGHS-1 (IC50= 20 uM). Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. Darbufelone mesylate was in phase III clinical trials by Pfizer and Zhuhai United Laboratories for the treatment of rheumatoid arthritis.
Status:
Investigational
Source:
NCT01556607: Phase 1 Interventional Completed Drug Safety
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
VP-14637 (also known as MDT 637) was developed as an inhibitor of respiratory syncytial virus (RSV). RSV is the leading cause of respiratory tract infections in humans. VP-14637 participated in phase I clinical trial to evaluate the safety and pharmacokinetic profile of the drug in healthy human volunteers. However, further study was discontinued because of the strategic decision.
Status:
Investigational
Source:
NCT00373516: Phase 2 Interventional Completed Psoriasis
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Becocalcidiol is a vitamin D analog participated in phase II clinical trials as a topical treatment for psoriasis. Therapy was safe and well tolerated, however further studies were discontinued.
