Name: Evofosfamide
CAS#: 918633-87-1
Chemical Formula: C9H16Br2N5O4P
Exact Mass: 446.93067
Molecular Weight: 449.04
Elemental Analysis: C, 24.07; H, 3.59; Br, 35.59; N, 15.60; O, 14.25; P, 6.90
Description: Evofosfamide, also known as TH-302, is a hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity. The 2-nitroimidazole moiety of hypoxia-activated prodrug TH-302 acts as a hypoxic trigger, releasing the DNA-alkylating dibromo isophosphoramide mustard moiety within hypoxic regions of tumors. Normoxic tissues may be spared due to the hypoxia-specific activity of this agent, potentially reducing systemic toxicity. Check for active clinical trials or closed clinical trials using this agent. (NCI).
Synonym: TH302; TH 302; TH-302. Evofosfamide
IUPAC/Chemical Name: Phosphorodiamidic acid, N,N'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester.
SMILES Code: O=P(NCCBr)(NCCBr)OCC1=CN=C([N+]([O-])=O)N1C
EOS Med Chem produce Evofosfamide,TH 302, 918633-87-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Evofosfamide,TH 302, 918633-87-1 Intermediates, EOS Med Chem have 8; Evofosfamide,TH 302, 918633-87-1 Impurity we have 10, all from GMP, FDA plant.
Now Evofosfamide,TH 302, 918633-87-1 DMF document is preparing.
Until 2016, Aug, Evofosfamide,TH 302, 918633-87-1 more than produced 25kg API, 120kg Intermediates
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Evofosfamide TH-302;HAP-302 918633-87-1
Evofosfamide Intermediates (1-methyl-2-nitro-1H-imidazol-5-yl)methanol 39070-14-9
Evofosfamide Intermediates N,N'-Bis(2-bromoethyl)phosphorodiamidic acid 141025-16-3
According to wikipedia.com, TH-302 is an experimental anticancer agent that is in clinical development at Threshold Pharmaceuticals, Inc. It is activated only at very low levels of oxygen (hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia. TH-302 exploits the activation of a nitroazole prodrug by a process that involves a one electron reduction mediated by ubiquitous cellular reductases such as the NADPH cytochrome P450 to generate a radical anion prodrug (RP). In the presence of oxygen (normoxia) the radical anion prodrug reacts rapidly with oxygen to generate the original prodrug and superoxide (SO). Under the low oxygen conditions of the hypoxic zones in tumors, however, the radical anion prodrug undergoes further irreversible reductions to the hydroxylamine (HA) followed by elimination, releasing the active drug and an azole derivative (AZ).
TH-302 started a Phase 1 clinical trial in 2007 in various solid tumors. The Phase 1 trial is a multi-center, open-label, dose-escalation study in patients with solid tumor cancers. The primary objectives of the study are to determine the maximum tolerated dose (MTD) and dose-limiting toxicities of TH-302 in patients with advanced solid tumors and to establish the appropriate dose to be tested in Phase 2 clinical trials. The secondary objectives of the trial include establishing the pharmacokinetics and assessing the anti-tumor activity of TH-302, as measured by objective response rate and duration of response, and to characterize the safety profile. Tumors will be evaluated at baseline and every eight weeks using the Response Evaluation Criteria In Solid Tumors (RECIST) criteria.
