Molecular Insight Pharmaceuticals, Inc announced the initiation of a phase-1 clinical trial of Solazed (Ioflubenzamide I-131), the company's targeted radiotherapeutic drug candidate for treatment of malignant metastatic melanoma. The phase-1 proof-of-concept study is being conducted with the University of Pennsylvania and is funded by a two-year grant from the National Cancer Institute that could total as much as US$ 1.5 million to support this stage of development of Solazed.

"Solazed is our fifth product candidate to enter the clinic, demonstrating our leadership in the development of molecular imaging and targeted radiotherapy of cancer," said Daniel L Peters, president and CEO of Molecular Insight. "We are hopeful that Solazed will offer a much-needed therapeutic option for patients with metastatic melanoma, a form of cancer known to be exceptionally difficult to treat and associated with a high level of morbidity and mortality."

"Targeting receptors over-expressed in cancers with radioactive payloads has the potential to be highly effective in both the in vivo detection and therapy of cancers," said Chaitanya R Divgi, professor of Radiology and chief, Nuclear Medicine and Clinical Molecular Imaging Section, University of Pennsylvania. "If fruitful, this method could fulfill an unmet need in melanoma, an aggressive cancer with few current effective therapies."

Solazed, a proprietary radiolabeled small molecule, was designed to bind to melanin found in melanomas and deliver a targeted and lethal dose of radiation to cancer cells through the radioactive decay of iodine-131. Melanin is a naturally occurring pigment that is over-expressed in about half of all melanoma tumours. The phase-1 clinical trial is designed to define the pharmacokinetics, normal organ distribution and radiation dosimetry of Solazed, and confirm localization in human melanomas. Researchers will image the distribution of Solazed in 12 patients with confirmed metastatic melanoma. Data from this study will inform the design of subsequent therapeutic dose-ranging studies.

In a nonclinical mouse model of human melanoma, Solazed administered in single or multiple doses significantly reduced tumour volumes for a prolonged period of time and enhanced survival compared to control groups treated with standard chemotherapy. In preclinical safety studies the compound exhibited an acceptable toxicity profile. Solazed was granted Orphan Drug status by the Food and Drug Administration for the treatment of stage 2B-4 metastatic melanoma in September 2008.