On April 3, 2019 Moleculin Biotech, Inc., (Nasdaq: MBRX) ("Moleculin" or the "Company"), a clinical stage pharmaceutical company with a broad portfolio of drug candidates targeting highly resistant tumors, reported that preclinical data supporting activity of its STAT3-inhibiting Immune/Transcription Modulators was presented by Dr. Waldemar Priebe, Founder and Chair of the Scientific Advisory Board of Moleculin, Inc. at the 2019 Annual Meeting of the American Association for Cancer Research (AACR) (Free AACR Whitepaper) ("AACR") in Atlanta, GA (Press release, Moleculin, APR 3, 2019, View Source [SID1234534948]).

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Please click the link below to view the Abstract for WP1066 and WP1732.

AACR Abstract:
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The presentation included data resulting from preclinical evaluation in pancreatic cancer models of STAT3 inhibitors WP1066 and WP1732, both discovered at The University of Texas MD Anderson Cancer Center and licensed by Moleculin. WP1066 is an orally bioavailable drug with significant brain uptake that is currently in Phase I clinical studies in patients with brain tumors. Complementary to WP1066, STAT3 inhibitor WP1732 is suitable for IV administration and demonstrates high uptake by the pancreas without uptake to the brain. In vitro efficacy of both inhibitors was assessed using proliferation and apoptosis induction assays in a panel of patient-derived and commercially-available Pancreatic Ductal Adenocarcinoma ("PDAC") cell lines. Both WP1066 and WP1732 were similarly potent and shown to induce apoptosis and inhibit p-STAT3 and its nuclear localization in all tested PDAC cell lines. Observed IC50 values ranged from 0.5 to 2 μM. WP1732 was well tolerated by mice (LD50 85 mg/kg given IV). Pharmacokinetic and biodistribution studies revealed very high uptake of WP1732 in the pancreas of mice and rats exceeding up to ~30 fold more than the drug levels in plasma. Importantly, both agents show in-vivo efficacy in preliminary experiments when tested alone or in combination with T cell immune checkpoint inhibitors.

The presentation concluded that WP1066 and WP1732 are inhibitors of p-STAT3 with demonstrated in vitro and in-vivo activity against PDAC tumor models, and that preliminary data warrant the further pre-clinical and clinical evaluation of these oncology agents alone and in combination with immunotherapy as promising new therapeutics for pancreatic cancer.

"The scientific community has been increasingly focused on inhibition of p-STAT3 as a new area for developing cancer therapies," commented Walter Klemp, Moleculin’s Chairman and CEO. "Our Immune/Transcription Modulators have a unique ability to both inhibit p-STAT3 and other key oncogenic transcription factors and to stimulate a natural immune response. We believe available preclinical data and the data presented at this AACR (Free AACR Whitepaper) Conference form a solid basis to pursue translational efforts for pancreatic cancer as one of our primary indications."