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Tucson, AZ, United States

Trademark
AmpliMed Corporation | Date: 2005-08-23

Pharmaceutical preparations for use in the treatment of cancer.


Trademark
AmpliMed Corporation | Date: 2005-08-23

Pharmaceutical preparations for use in the treatment of cancer.


Trademark
AmpliMed Corporation | Date: 2006-08-25

Pharmaceutical preparations for use in the treatment of cancer.


Remers W.A.,AmpliMed Corporation | Remers W.A.,Arizona Cancer Center | Remers W.A.,AmplMed Corporation | Dorr R.T.,AmpliMed Corporation | And 2 more authors.
Current Medicinal Chemistry | Year: 2012

Following the demonstration that addition of a 2-cyano group to aziridines prevented DNA alkylation and thus reduced toxicity, many novel 2-cyanoaziridines were synthesized and evaluated as immunomodulating and antitumor agents. They typically reacted with thiols such as cysteine, depleting them and allowing the accumulation of reactive oxygen species. Two of these compounds, azimexon and ciamexon, showed activity against tumors in clinical trials. Imexon was produced by cyclization of 2-cyanoaziridine-1-carboxamide in the presence of hydroxide ions. The two enantiomers were prepared by a process involving chiral chromatography. They were equipotent against cultured tumor cells. Imexon also reacts with thiols and it is especially potent against multiple myeloma in cell cultures. An efficient chemical synthesis and a lyophilization formulation of imexon as a water soluble, injectible drug, were developed. In Phase I and I/II clinical trials imexon showed hints of activity against a variety of tumors, but a randomized double-blind Phase II trial of imexon plus gemcitabine versus gemcitabine alone in pancreatic cancer showed no enhancement of activity above that of gemcitabine alone. This result was disappointing because in cell culture and mice the two compounds were synergistic. Based on a complete response in a Phase I trial, a new Phase II clinical trial of imexon is underway in non-Hodgkins lymphoma. © 2012 Bentham Science Publishers. Source


Cohen S.J.,Chase Medical | Zalupski M.M.,University of Michigan | Modiano M.R.,Arizona Clinical Research Center | Conkling P.,Us Oncology Phase I Group | And 7 more authors.
Cancer Chemotherapy and Pharmacology | Year: 2010

Purpose: Imexon is an aziridine-derived iminopyrrolidone which has synergy with gemcitabine in pancreatic cancer cell lines. Gemcitabine is a standard therapy for pancreatic cancer. We performed a phase I trial of imexon and gemcitabine to evaluate safety, dose-limiting toxicity (DLT), and maximum tolerated dose (MTD) in patients with advanced pancreatic cancer. Methods: Patients with untreated locally advanced or metastatic pancreatic adenocarcinoma received therapy in sequential cohorts on regimen A (n = 19; imexon 200 or 280 mg/m2 intravenously (IV) over 30 min days 1-5, 15- 19 and gemcitabine 800 or 1,000 mg/m2 IV over 30 min on days 1,8,15 every 28 days) or regimen B (n = 86; imexon 280-1,300 mg/m2 IV over 30-60 min days 1, 8, and 15 and gemcitabine 1,000 mg/m2 IV over 30 min on days 1, 8, and 15 every 28 days). Results: One hundred five patients received 340 treatment cycles (median 2, range 1-16). Patient characteristics: median age 63, 61% male, ECOG PS 0/1 50%/50%, 93% metastatic. DLT was abdominal cramping and pain, often with transient, acute diarrhea. Best response was confirmed partial response (PR) in 11.4%, 8.9% unconfirmed PR, and 48.1% with stable disease. There was a dose proportional increase in imexon AUC across the doses tested with terminal half life 69 min at the MTD and no alteration of gemcitabine pharmacokinetics. Conclusions: The recommended phase II dose of imexon is 875 mg/m2 with gemcitabine 1,000 mg/m2. DLT was acute abdominal pain and cramping. Encouraging antitumor responses support further evaluation of this combination in advanced pancreatic cancer. Source

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