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TT-232 is a structural analogue of somatostatin, an endogenous hormone with significant, selective antiproliferative, anti-inflammatory and antisecretory properties. In contrast to the parent hormone and its “traditional” analogues, this compound has strong and specific growth-inhibitory potential without the wide-ranging endocrine side-effects, including inhibition of insulin secretion provoking diabetes. The molecule has been shown to have unique conformational characteristics, selective binding properties to the 1st and 4th subtypes of somatostatin receptors (SSTR1 and 4) and to the intracellular receptor pyruvate kinase M2. No presently marketed drug or drug-candidate in clinical trials has a comparable molecular mechanism and efficacy profile on these new pharmaceutical drug-targets in the therapy of inflammation. Its mechanism of action is in line with a new era of molecular medicine called signal-transduction therapy, where "internal communication" of cells is corrected without interfering with basic cell functions and machinery. This relatively new concept has proven success with a real “block-buster”, Gleevec® (Novartis) in chronic myeloid leukaemia, where revenues reached $600 million last year, expected to exceed a billion USD in 2003 according to recent market prognosis.

Historically, development of TT-232 was started as a signal-transduction inhibitor drug candidate targeting oncological applications in 1993, while increasing evidence on the molecular pharmacology of its action along with extensive preclinical efficacy studies have put the anti-inflammatory indication also into the front line of present development efforts. The preclinical dossiers in both indications have been completed. Primary oncological disease targets were set to malignant melanoma (MM), breast cancer (BC) and chronic lymphoid leukaemia (CLL). After successful phase I clinics on healthy volunteers, the first human phase II (safety and dose-finding efficacy) trial using TT-232 as a single agent in late stage disseminated MM was completed. This confirmed predicted safety and showed promising clinical response. Add-on trials on MM and BC are in progress and under preparation, respectively.

The overall results of the numerous safety studies showed that TT-232 is a molecule of low toxicity: no accumulation, allergic or mutagenic effects were seen. The most significant feature is that TT-232 does not affect vital function or morphology of tissues as most cytotoxic agents used in the baseline treatment of inflammatory disorders (e.g. methotrexate in rheumatoid arthritis) and classical anticancer agents do. Minor side effects like hypotension and some local reactions after intravenous administration in peripheral vessels did not require medical attention.

TT-232 has been shown to be a potent neurogenic inflammation inhibitory, anti-inflammatory and analgesic agent with a broader spectrum than presently available anti-inflammatory/analgesic drugs. In animal models it is effective against neurogenic inflammation and blocks neuropathic hyperalgesia where COX-1 or COX-2 inhibitors (e.g. diclofenac or meloxicam) proved ineffective. Predicted indication profile of TT-232 is in line with “disease-modifying” agents in the baseline therapy of “autoimmune” inflammatory disorders, where classical anticancer agents have proven success in the past 20 years (see methotrexate, azathioprine, etc.). Acting on the peripheral sensory neurons, this molecule has a strong analgesic effect too, which proved significantly greater than that of non-steroid anti-inflammatory agents (e.g. diclofenac) and comparable to morphine in various animal models. After completed human phase I safety trials, phase II clinical studies are now planned in two of the most promising disease indications, rheumatoid arthritis and burn injuries.

All pre-clinical and clinical studies were performed according to international standards (GLP, GMP & GCP) in conform with European and FDA ICH requirements. Development until now was funded in three financing rounds with a significant amount of R&D grants.