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Piqur.ch

B I O T E C H ’ S M O S T R E S P E C T E D N E W S S O U R C E F O R M O R E T H A N 2 0 Y E A R S
Tygacil by the Tail? Tetraphase
Partnering Your Way to M&A?
IPO: $86M for New Antibiotics
Keep Cash Balance, Options
Looking to bolster its planned Phase III trial with TP-434 NEW YORK – How does a biotech company look to set (eravacycline) for complicated intra-abdominal infections, itself up as a potential acquisition target down the road? Tetraphase Pharmaceuticals Inc. fi led for an initial public The answer, according to a panel at this year’s BIO CEO & offering (IPO) that would raise up to $86.2 million, though Investor Conference, is that it depends. neither the targeted number of shares nor the price of each On fi nancing, on the indications, the market size In February 2012, the company landed a $67 million Heard it at
federal contract for the broad-spectrum antibiotic from the #BIOCEO13, p. 9
Biomedical Advanced Research and Development Authority, which came six months after a $36 million National Institutes One, the number of M&A deals has dropped in the past of Health (NIH) contract for a separate, respiratory antibiotic, Only one new compound in the tetracycline class, StemCells: Spinal Injury Gains
Tygacil (tigecycline, Pfi zer), has been approved in more than 30 years, mainly because semi-synthetic production Are Sustained After One Year
methods hinder chemical diversity. Tetraphase’s approach TP-434 is a fully synthetic tetracycline antibiotic, created StemCells Inc. reported positive results from the fi rst using Watertown, Mass.-based Tetraphase’s tetracycline patient cohort of a Phase I/II trial of its human neural chemistry platform, licensed from Harvard University. stem cell product for spinal cord injury, and investors Positive Phase II data were unveiled in September 2012.
responded enthusiastically, driving the Newark, Calif.- Intended for Gram-negative and Gram-positive pathogens, TP-434 targets bugs such as Escherichia coli Out of three patients with complete, chest-level spinal and Klebsiella pneumonia, in the former category, as well injury, two had regained sensitivity to heat, touch and N e w C o N e w s
Lycera Expands Partnership
With Merck for Potential $600M
Swiss Start-up Piqur Developing
Dual PI3K-mTOR Inhibitors
Lycera Corp. doubled its sweet 2011 deal with Merck and Co. Inc., of Whitehouse Station, N.J., in a new agreement designed to expand on the companies’ prior Matthias Wymann, the Swiss scientist who discovered relationship, which has centered on retinoic acid-related the fi rst phosphoinositide 3-kinase (PI3K) inhibitor, is co- orphan receptor (ROR[gamma]t). Lycera will receive an founder of a new cancer drug discovery start-up, Piqur undisclosed up-front payment and research funding, OTHER NEWS TO NOTE: ONCOCEUTICS, ORAGENICS, OXYGEN .7 INSIDE: PHARMA OTHER NEWS TO NOTE: NOVO NORDISK, DR. REDDY’S .9
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Copyright 2013 AHC Media. Reproduction is strictly prohibited. Visit our web site at www.bioworld.com unwanted activation of PI3K signaling. Yet some level of mTOR inhibition has a synergistic effect on shutting down Therapeutics AG, which recently completed a seed fi nancing round that will enable it take forward a pipeline of next- Piqur has identifi ed what it believes will be fi nely tuned dual inhibitors that do not reactivate the PI3K signal.
The company, a spinout from the University of Basel, “We call it balanced inhibition. We think effi cacy can be where Wymann is based, is developing dual inhibitors of improved if you have a balanced way of inhibiting the two PI3K and mammalian target of rapamycin (mTOR). It has assembled a veritable who’s who of scientifi c staff and The company has also opted to focus on dual inhibitors advisers, who have played leading roles in the development with pan-PI3K selectivity in order to maximize their The other co-founders include company chairman Drugs that target only one of the four Class I PI3K Bernd Giese, a high-profi le organic chemist best known for isoforms that are important in cancer, such as GS-1101 (CA- his work on electron charge transfer in DNA and peptides; 101), the Phase III PI3K delta inhibitor Foster City, Calif.- CEO Vladimir Cmiljanovic, who spent his scientifi c research based Gilead Sciences Inc. acquired in its takeover of career with Giese and Wymann; and Andreas Emmenegger, Calistoga Pharmaceuticals, have more limited application. chief fi nancial offi cer of Molecular Partners AG, of Zurich, “All isoforms are involving in cancer signaling pathways,” Switzerland. Its chief scientifi c offi cer is Doriano Fabbro, formerly head of kinase biology at Novartis AG, of Basel, Although Piqur’s kinase inhibitors can act on all four Switzerland. Its scientifi c advisory board includes Michael PI3Ks, as well as the two kinase activities present in the two Hall, of the University of Basel, who discovered TOR.
mTOR complexes, they do not appear to affect the hundreds About 20 years ago, Wymann identifi ed PI3K as the of other kinases that are involved in myriad signaling roles. target of wortmannin, a fungal metabolite known for “We know that our front-runner compound doesn’t have inhibiting respiratory burst (or oxidative burst) activity in specifi c off-target activities according to the preclinical neutrophils. (Seattle-based Oncothyreon Inc. is conducting compound characterization,” Cmiljanovic said.
Phase II trials in multiple cancer indications of a semi- Piqur – the name is a play on PI3K, the concept that one in three people have a lifetime risk of developing cancer and Over the past decade, Wymann and his team have the notion of a cure for cancer – has not disclosed the size assisted several large pharma fi rms in the discovery and of its initial funding round. Its investors are high-net worth development of PI3K-Akt-mTOR pathway inhibitors. The individuals with signifi cant experience in the life sciences pathway plays an important role in down-regulating industry. The funding will enable the company to advance apoptosis and prolonging cell survival. Aberrant signaling its operational set-up, complete preclinical development of or amplifi cation of the pathway is a signifi cant feature of its lead compound, PQR-309, and prepare for its fi rst clinical trial, which could commence later this year. ■ BEZ235 was the fi rst dual inhibitor of PI3K and mTOR to reach the clinic. Novartis is now conducting Phase II Other News To Note
trials of the compound in multiple cancer indications. Paris-based Sanofi SA is also in the clinic with a dual inhibitor, SAR245409 (XL765), which it in-licensed from Exelexis Inc., • MiReven, of Perth, Western Australia, reported the publication of an in vitro study where the microRNA miR- Piqur has identifi ed a series of compounds with attractive 7-5p signifi cantly inhibited the migration and invasion of profi les using high-throughput screening, combined with in metastatic melanoma cells in the journal Biochemical and silico modeling and X-ray crystallographic analysis. Biophysical Research Communications. In the study, miR- “What Piqur has today are molecules, which have 7-5p expression was shown to be reduced in metastatic signifi cantly improved physico-chemical properties, leading melanoma-derived cell lines compared with primary to the improved pharmacological properties,” Cmiljanovic melanoma cells. When the microRNA was reintroduced and expressed ectopically, migration and invasion of the The compounds exhibit strong PI3K inhibition and melanoma cells was signifi cantly inhibited in vitro. The weaker mTor inhibition, in contrast to BEZ235, a compound study authors also investigated the mechanism of miR- which some of the Piqur team worked on during its 7-5p and found that insulin receptor substrate-2 (IRS-2) preclinical characterization. “BEZ235 is a stronger mTor is a functional target of miR-7-5p, which then decreases inhibitor than it is a PI3 kinase inhibitor,” Cmiljanovic said. activity in the protein kinase B (Akt) signaling pathway, a However, excessive mTOR inhibition leads to the loss key regulator of many oncogenic processes including cell of negative feedback loop, which, ultimately, leads to an To subscribe, please call BIOWORLD® Customer Service at (800) 477-6307; outside the U.S. and Canada, call (404) 262-5476.
Copyright 2013 AHC Media. Reproduction is strictly prohibited. Visit our web site at www.bioworld.com

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