Brostallicin Press Kit
Potentially More Patient-friendly
Brostallicin (bräst-al-iss-in) is a small molecule, anti-cancer drug with a novel and unique mechanism of action and excellent long-term patent protection. Data in more than 200 patients treated in phase I/II clinical trials reveal evidence of activity in patients with refractory cancer and patient/physician-friendly dosage and administration. Brostallicin may ultimately be useful in combination with standard chemotherapy and newer, targeted cancer therapies.
A New Class of Cancer Drug
Brostallicin is a new class of cancer drug — a synthetic DNA minor groove binding agent. Most cytotoxic agents bind DNA’s major groove, have little sequence-specificity, and are severely toxic to normal tissues (including topoisomerase inhibitors, such as camptothecins and anthracyclines).
DNA minor groove binders such as brostallicin possess high affinity and selectivity for interaction with DNA. All minor groove binders bind to the same DNA structure; however, brostallicin has a unique and very interesting mechanism of action.
A Novel and Unique Mechanism of Action
Brostallicin binds to DNA only in the presence of glutathione (GSH) and glutathione S-transferase (GST), which are overexpressed in cancer cells, but not in normal cells.
This gives brostallicin a novel and highly selective mechanism of action that is superior to other minor groove binding agents.
By binding to the minor groove, brostallicin provides a new target to interfere with DNA division and lead to tumor cell death. Brostallicin is potently synergistic in combination with standard cytotoxic agents as well as newer targeted therapies.
High Anti-cancer Activity
Brostallicin has a unique ability to become more active in tumors that are resistant to other cancer drugs. Its anti-tumor activity remains high in the presence of a number of critical cancer causing genetic abnormalities that cause resistance to standard anti-cancer agents. This activity profile makes it of extreme interest in designing trials to test its activity in targeted patients with certain genetic abnormalities.
Brostallicin Clinical Research
Brostallicin is currently in phase II clinical trials versus doxorubicin as first-line single-agent chemotherapy in patients with advanced or metastatic soft tissue sarcoma. The European Organization for Research and Treatment of Cancer (EORTC) Soft Tissue and Bone Sarcoma Group completed a phase II trial of brostallicin, concluding that brostallicin met their criteria for continued development (47 percent of patients were progression-free at three months). EORTC’s phase II follow-up trial in sarcoma is currently ongoing.
In late 2007, we also initiated a phase II trial of brostallicin for the treatment of myxoid liposarcoma.
