Biotica achieves preclinical proof-of-concept in nPT-CLN asthma programme
Cambridge UK: 2 October 2009
Biotica, the leader in discovery of polyketide therapeutics, today announces that it has reached preclinical proof-of-concept in its nPT-CLN programme for the treatment of severe asthma. Following this achievement, Biotica is now seeking a partner with expertise in inhalation and/or respiratory disease to develop and commercialise nPT-CLN compounds.
Compounds in the nPT-CLN series inhibit calcineurin (CLN), a protein which stimulates components of the immune system associated with asthma. Biotica applied its novoPT™ technology to create novel analogues of the well-understood CLN inhibitor tacrolimus (FK506), a powerful immune suppressant. FK506 itself is active in asthma patients, and has been shown to be active in tissues taken from steroid-resistant patients. However, it has some undesirable side-effects when used systemically that prevent it being used clinically in asthma.
The nPT-CLN compounds retain potent CLN inhibition but have minimal systemic bioavailability. Biotica’s preclinical proof-of-concept studies establish that the compounds exhibit minimal systemic inhibition of CLN because they are rapidly converted to a relatively inactive form. When given by inhalation, exposure to the compounds in the lung is several orders of magnitude higher than in the blood. This means that the compounds will exert their anti-inflammatory effect in the lungs, but will not have the side-effects associated with systemic exposure to calcineurin inhibitors.
Biotica is positioning the nPT-CLN compounds for use in severe asthma, which includes up to 20% of the patient population. These patients are not well treated by steroid-based therapies. Combined with the severity of the symptoms, the lack of treatment options for severe asthma makes it an indication of high clinical need.
Biotica Technology Ltd
Dr Edward E. Hodgkin, CEO
Tel: +44 1799 532920
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About calcineurin inhibition and asthma
Calcineurin (CLN) stimulates production of pro-inflammatory cytokines and activates T-cells. In asthma, overproduction of cytokines stimulates chronic lung inflammation. Furthermore, the lungs of asthma patients have elevated numbers of T-cells, and T-cell activation correlates with asthma severity. Inhibiting CLN using FK506 has been shown clinically to have activity in asthma patients. FK506 has also been shown to inhibit T-cell activation in steroid-resistant tissues from asthma patients, supporting the positioning of nPT-CLN for patients with severe asthma.
About Biotica
Biotica is a privately-held biotechnology company that discovers and develops polyketide therapeutics. It has a growing pipeline of novel therapeutic programmes supported by clinical validation. These include nPT-mTOR (unique mTOR inhibitors partnered with Wyeth), nPT-CLN (potent calcineurin inhibitors for inhaled use in asthma), nPT-CyP (cyclophilin inhibitors for HCV) and nPT-ery (erythromycin analogues partnered with GlaxoSmithKline). All of Biotica’s projects employ its proprietary novoPT™ technology, which enables it to select from the many known polyetides with biological activity and make a range of derivatives that are either difficult or impossible to make by medicinal chemistry methods. For additional information visit http://www.biotica.com