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ANACOR CLINICAL STUDY OF AN2728, A NOVEL ANTI-INFLAMMATORY COMPOUND, SHOWS
EFFICACY IN PSORIASIS
-- Topical Therapy Reduces TNF-alpha Production Through Inhibition of PDE-4 Enzyme --
Palo Alto, Calif. - June 6, 2007 - Anacor Pharmaceuticals, a privately held pharmaceutical company,
announced today the results from its placebo-controlled Phase 1 trial of AN2728, a first-in-class topical therapy under
investigation for the treatment of psoriasis. The trial showed AN2728 to be well-tolerated, with activity comparable
to existing topical treatments for psoriasis.
AN2728 is the product of a focused medicinal chemistry effort to create small molecules that inhibit TNF-alpha, the
inflammatory cytokine that is the target of the powerful monoclonal antibodies now marketed for the treatment of
psoriasis. Company researchers have shown that AN2728 suppresses the phosphodiesterase 4 (PDE4) enzyme, leading to
TNF-alpha inhibition.
"This early-stage trial demonstrated definitive anti-inflammatory activity in humans. We are encouraged that the
compound decreases TNF-alpha, a cytokine known to be important in psoriasis, by the inhibition of PDE4, a well-validated
anti-inflammatory target," said Karl Beutner, Anacor's chief medical officer. "A topical compound that effectively
targets TNF-alpha would have great promise, and we intend to initiate further clinical trials to characterize the
clinical utility of this drug in psoriasis and other inflammatory skin diseases."
Psoriatic plaques on each of the 12 patients enrolled in the trial were divided into six sections, and each of
those sections was treated with a different therapy: AN2728 ointment, AN2728 cream, betamethasone, tacrolimus
(Protopic) and vehicle cream and ointment. Using ultrasound, researchers measured the thickness of the inflammatory
infiltrate in the psoriatic plaques and also recorded the clinical response based on an investigator global evaluation
of disease severity.
As measured by decreases in the thickness of the infiltrate and clinical scores, AN2728-treated plaques improved
significantly compared with vehicle treatment (p<0.001), and efficacy was comparable to that seen with
betamethasone and tacrolimus. AN2728 treatment was well-tolerated in all patients.
About Psoriasis
Psoriasis is an inflammatory skin disorder that affects approximately 14 million individuals worldwide. The
disorder ranges from a single, small, localized lesion in some patients to a severe, disfiguring skin condition
that may be associated with disabling arthritis.
About Anacor Pharmaceuticals
Anacor, a privately held, clinical-stage pharmaceutical company, is developing novel product candidates for
inflammatory, fungal and bacterial diseases based on its proprietary, small-molecule, boron-based chemistry.
The company's lead product is AN2690, which is in Phase 2 trials for onychomycosis, a fungal infection of the
nail and nailbed. Anacor has entered into an exclusive, worldwide agreement with Schering-Plough Corporation to
develop and commercialize the drug. The company is also conducting clinical trials with two anti-inflammatory
product candidates, AN2728 and AN0128.
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