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Restrict the search for
uracil mustard
to a specific field?
Status:
US Approved Rx
(2012)
Source:
NDA203923
(2012)
Source URL:
First marketed in 1921
Source:
Sodium Thiosulphate U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sodium thiosulfate (sodium thiosulphate/STS) is a chemical and medication. As a medication, it is used in combination with sodium nitrite under the trade name to NITHIODOTE treat cyanide poisoning. The primary route of endogenous cyanide detoxification is by enzymatic transulfuration to thiocyanate (SCN- ), which is relatively nontoxic and readily excreted in the urine. Sodium thiosulfate is thought to serve as a sulfur donor in the reaction catalyzed by the enzyme rhodanese, thus enhancing the endogenous detoxification of cyanide. In addition, Sodium thiosulfate is used in calciphylaxis in hemodialysis patients with end-stage kidney disease. Calciphylaxis is vasculopathy characterized by ischemia and painful skin necrosis due to calcification and intimal fibroplasia of thrombosis of the panicular arterioles. Sodium thiosulfate is used as treatment due to its antioxidant activity and as a chelating. Sodium thiosulfate renders renal protection by modulating the mitochondrial KATP channel for preventing urolithiasis. Moreover, STS was assumed to play a vital role in on ischemia reperfusion injury (IR). The effectiveness of STS as a cardioprotective agent was attributed to the reduction of apoptosis by binding to the active site of caspase-3 in silico, which was substantiated by the reduced expression of caspase-3 and poly ADP ribose polymerase levels.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mannomustine is a substance synthesized as one of a series of compounds linking the actively cytotoxic chemical group beta-chlorethylamine with a naturally
occurring substance, mannitol. Mannomustine is an alkylating agent with antineoplastic properties. It was being studied in the treatment of hematologic malignancies.
Status:
Investigational
Source:
NCT02073838: Phase 2 Human clinical trial Completed Leukemia, Myeloid, Acute/genetics/metabolism
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT02073838: Phase 2 Human clinical trial Completed Leukemia, Myeloid, Acute/genetics/metabolism
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT01168791: Phase 3 Interventional Completed Soft Tissue Sarcoma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Palifosfamide or ZIO-201 (isophosphoramide mustard; IPM), a bi-functional DNA alkylator, is the active metabolite of ifosfamide (IFOS). IFOS and the related drug cyclophosphamide (CPA) are widely used anti-cancer drugs. Both are pro-drugs and need to be metabolized to be active. Their clinical use is limited by the toxicity associated with some of their metabolites. Palifosfamide has shown efficacy in diverse cancer models. ZIOPHARM Oncology Inc, under license from Dekk-Tec Inc, was developing palifosfamide, a formulation of isophosphoramide mustard with tris(hydroxymethyl)aminomethane salt-stabilization (palifosfamide-tris) and previously with lysine-stabilization (palifosfamide-lys). Preclinical studies and phase I and I/II clinical trials demonstrated that palifosfamide-tris had an antitumor efficiency comparable or superior to that of ifosfamide. To date ZIO-201 is not present in ZIOPHARM pipeline.
Status:
Investigational
Source:
NCT00102973: Phase 3 Interventional Completed Ovarian Neoplasms
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Canfosfamide is a modified glutathione analogue and nitrogen mustard prodrug, with potential antineoplastic activity. Canfosfamide is selectively activated by glutathione S-transferase P1-1 an enzyme that is over-expressed in many human cancers including ovarian cancer. GST P1-1-mediated cleavage leads to an active cytotoxic phosphorodiamidate alkylating metabolite that forms covalent linkages with nucleophilic centers in tumor cell DNA, which may induce a cellular stress response and cytotoxicity, and decrease tumor cell proliferation. Preclinical studies showed that canfosfamide inhibited the growth and was cytotoxic to a wide range of established cancer cell lines including those derived from ovarian cancer (OVCAR3, HEY, SK-OV-3). Canfosfamide treatment inhibited cancer cell proliferation and induced apoptosis through the activation of the cellular stress response kinase pathway. The cytotoxic activity of canfosfamide correlated with the expression of GST P1-1. Cancer cells in which GST expression levels were increased by transfection with the GST P1-1 gene, were more sensitive to the cytotoxic effects of canfosfamide than the parental cell lines Canfosfamide in combination with pegylated liposomal doxorubicin is well tolerated and active in platinum and paclitaxel refractory or resistant ovarian cancer.
Status:
Investigational
Source:
NCT00102973: Phase 3 Interventional Completed Ovarian Neoplasms
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Canfosfamide is a modified glutathione analogue and nitrogen mustard prodrug, with potential antineoplastic activity. Canfosfamide is selectively activated by glutathione S-transferase P1-1 an enzyme that is over-expressed in many human cancers including ovarian cancer. GST P1-1-mediated cleavage leads to an active cytotoxic phosphorodiamidate alkylating metabolite that forms covalent linkages with nucleophilic centers in tumor cell DNA, which may induce a cellular stress response and cytotoxicity, and decrease tumor cell proliferation. Preclinical studies showed that canfosfamide inhibited the growth and was cytotoxic to a wide range of established cancer cell lines including those derived from ovarian cancer (OVCAR3, HEY, SK-OV-3). Canfosfamide treatment inhibited cancer cell proliferation and induced apoptosis through the activation of the cellular stress response kinase pathway. The cytotoxic activity of canfosfamide correlated with the expression of GST P1-1. Cancer cells in which GST expression levels were increased by transfection with the GST P1-1 gene, were more sensitive to the cytotoxic effects of canfosfamide than the parental cell lines Canfosfamide in combination with pegylated liposomal doxorubicin is well tolerated and active in platinum and paclitaxel refractory or resistant ovarian cancer.
Status:
Designated
Source:
FDA ORPHAN DRUG:354611
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
AEOL-10150 is a small-molecule antioxidant developed by Aeolus (formerly Incara) for potential subcutaneous treatment for amyotrophic lateral sclerosis (ALS), stroke, spinal cord injury, lung inflammation, and mucositis. Structurally, AEOL-10150 functions as a superoxide-dismutase mimic and contains metalloporphyrin moiety. AEOL-10150 possess high superoxide-dismutase activity as well as catalase-like activity and has the capacity to scavenge peroxynitrite and lipid peroxides. In 2017 Aeolus Pharmaceuticals has announced that the FDA has granted Fast Track designation to AEOL 10150 for the prevention of fatal respiratory failure among patients at risk for radiation pneumonitis following a radiological/nuclear incident sufficient to cause the Acute Radiation Syndrome.