[2015-Feb-13] FDA approves Lenvima for a type of thyroid cancer

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm434288.htm

Lenvima.cdx

Junji Matsui, Yasuhiro Funahashi, Toshimitsu Uenaka, Tatsuo Watanabe, Akihiko Tsuruoka and Makoto Asada, Multi-Kinase Inhibitor E7080 Suppresses Lymph Node and Lung Metastases of Human Mammary Breast Tumor MDA-MB-231 via Inhibition of Vascular Endothelial Growth Factor-Receptor (VEGF-R) 2 and VEGF-R3 Kinase, Clin. Cancer Res., 2008, 14 (17), pp 5459-5465

http://dx.doi.org/10.1158/1078-0432.CCR-07-5270

Haizhen Zhong and J. Phillip Bowen, Recent Advances in Small Molecule Inhibitors of VEGFR and EGFR Signaling Pathways, Curr. Top. Med. Chem., 2011, 11 (12), pp 1571-1590

http://dx.doi.org/10.2174/156802611795860924

[2015-Feb-03] FDA approves Ibrance for postmenopausal women with advanced breast cancer

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm432871.htm

ibrance.cdx

David W. Fry, Patricia J. Harvey, Paul R. Keller, William L. Elliott, MaryAnne Meade, Erin Trachet, Mudher Albassam, XianXian Zheng, Wilbur R. Leopold, Nancy K. Pryer and Peter L. Toogood, Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts, Mol. Cancer Ther., 2004, 3 (11), pp 1427-1437

http://mct.aacrjournals.org/content/3/11/1427.abstract

Peter L. Toogood, Patricia J. Harvey, Joseph T. Repine, Derek J. Sheehan, Scott N. VanderWel, Hairong Zhou, Paul R. Keller, Dennis J. McNamara, Debra Sherry, Tong Zhu, Joanne Brodfuehrer, Chung Choi, Mark R. Barvian, and David W. Fry, Discovery of a Potent and Selective Inhibitor of Cyclin-Dependent Kinase 4/6, J. Med. Chem., 2005, 48 (7), pp 2388–2406

http://dx.doi.org/10.1021/jm049354h

Michal Marzec, Monika Kasprzycka, Raymond Lai, Andrew B. Gladden, Pawel Wlodarski, Ewa Tomczak, Peter Nowell, Samuel E. DePrimo, Seth Sadis, Stephen Eck, Stephen J. Schuster, J. Alan Diehl, and Mariusz A. Wasik, Mantle cell lymphoma cells express predominantly cyclin D1a isoform and are highly sensitive to selective inhibition of CDK4 kinase activity, Blood, 2006, 108 (5), pp 1744-1750

http://dx.doi.org/10.1182/blood-2006-04-016634

Raya Saab, Jennifer L. Bills, Alexander P. Miceli, Colleen M. Anderson, Joseph D. Khoury, David W. Fry, Fariba Navid, Peter J. Houghton and Stephen X. Skapek, Pharmacologic inhibition of cyclin-dependent kinase 4/6 activity arrests proliferation in myoblasts and rhabdomyosarcoma-derived cells, Mol. Cancer Ther., 2006, 5 (5), pp 1299-1308

http://dx.doi.org/10.1158/1535-7163.MCT-05-0383

Richard S. Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J. Cohen, Amrita J. Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los and Dennis J. Slamon, PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro, Breast Cancer Res., 2009, 11 (5), R77

http://dx.doi.org/10.1186/bcr2419

[2015-Jan-30] FDA approves Glyxambi for adults with type 2 diabetes

http://us.boehringer-ingelheim.com/news_events/press_releases/press_release_archive/2015/2-2-2015-us-fda-approves-first-in-class-glyxambi-empagliflozin-linagliptin-tablets-adults-type-2-diabetes.html

Glyxambi.cdx

R. Grempler, L. Thomas, M. Eckhardt, F. Himmelsbach, A. Sauer, D. E. Sharp, R. A. Bakker, M. Mark, T. Klein and P. Eickelmann, Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors, Diabetes Obes. Metab., 2012, 14 (1), pp 83-90

http://dx.doi.org/10.1111/j.1463-1326.2011.01517.x

Matthias Eckhardt, Elke Langkopf, Michael Mark, Moh Tadayyon, Leo Thomas, Herbert Nar, Waldemar Pfrengle, Brian Guth, Ralf Lotz, Peter Sieger, Holger Fuchs and Frank Himmelsbach, 8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a Highly Potent, Selective, Long-Acting, and Orally Bioavailable DPP-4 Inhibitor for the Treatment of Type 2 Diabetes, J. Med. Chem., 2007, 50 (26), pp 6450–6453

http://dx.doi.org/10.1021/jm701280z

[2015-Jan-08] FDA approves anti-clotting drug Savaysa

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm429523.htm

Savaysa.cdx

T. Furugohri, K. Isobe, Y. Honda, C. Kamisato-Matsumoto, N. Sugiyama, T. Nagahara, Y. Morishima, and T. Shibano, DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles, J. Thromb. Haemost., 2008, 6(9), 1542–1549

http://dx.doi.org/10.1111/j.1538-7836.2008.03064.x

[2014-Dec-19] FDA approves Rapivab to treat flu infection

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm427755.htm

Rapivab.cdx

Y. Sudhakar Babu, Pooran Chand, Shanta Bantia, Pravin Kotian, Ali Dehghani, Yahya El-Kattan, Tsu-Hsing Lin, Tracy L. Hutchison, Arthur J. Elliott, Cynthia D. Parker, Sandya L. Ananth, LaShun L. Horn, Graeme W. Laver, and John A. Montgomery, BCX-1812 (RWJ-270201): Discovery of a Novel, Highly Potent, Orally Active, and Selective Influenza Neuraminidase Inhibitor through Structure-Based Drug Design, J. Med. Chem., 2000, 43 (19), pp 3482-3486

http://dx.doi.org/10.1021/jm0002679

[2014-Dec-19] FDA approves new antibacterial drug Zerbaxa

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm427534.htm

Zerbaxa.cdx

Shinobu Takeda, Toru Nakai, Yoshimi Wakai, Fumiaki Ikeda and Kazuo Hatano, In Vitro and In Vivo Activitiesof a New Cephalosporin, FR264205, against Pseudomonas aeruginosa, Antimicrob. Agents Chemother., 2007, 51 (3), pp 826-830

http://dx.doi.org/10.1128/AAC.00860-06

David J. Payne, Rebecca Cramp, David J. Winstanley and David J. C. Knowles, Comparative activities of clavulanic acid, sulbactam, and tazobactam against clinically important beta-lactamases. Antimicrob. Agents Chemother., 1994, 38 (4), pp 767-772

http://dx.doi.org/10.1128/AAC.38.4.767

Efthimios E. Prinarakis, Vivi Miriagou, Eva Tzelepi, Maria Gazouli and Leonidas S. Tzouvelekis, Emergence of an inhibitor-resistant beta-lactamase (SHV-10) derived from an SHV-5 variant, Antimicrob. Agents Chemother., 1997, 41 (4), pp 838-840

http://aac.asm.org/content/41/4/838.abstract

H. Bermudes, F. Jude, E. B. Chaibi, C. Arpin, C. Bebear, R. Labia, and C. Quentin, Molecular Characterization of TEM-59 (IRT-17), a Novel Inhibitor-Resistant TEM-Derived β-Lactamase in a Clinical Isolate of Klebsiella oxytoca, Antimicrob. Agents Chemother., 1999, 43 (7), pp 1657-1661

http://aac.asm.org/content/43/7/1657.abstract

E. B. Chaïbi, D. Sirot, G. Paul and R. Labia, Inhibitor-resistant TEM β-lactamases: phenotypic, genetic and biochemical characteristics, J. Antimicrob. Chemother., 1999, 43 (4), pp 447-458

http://dx.doi.org/10.1093/jac/43.4.447

Youjun Yang, Beth A Rasmussen, David M Shlaes, Class A β-lactamases—enzyme-inhibitor interactions and resistance, Pharmacol. Ther., 1999, 83 (2), pp 141-151

http://dx.doi.org/10.1016/S0163-7258(99)00027-3

[2014-Dec-19] FDA approves Viekira Pak to treat hepatitis C

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm427530.htm

Viekira Pak.cdx

David A. DeGoey, John T. Randolph, Dachun Liu, John Pratt, Charles Hutchins, Pamela Donner, A. Chris Krueger, Mark Matulenko, Sachin Patel, Christopher E. Motter, Lissa Nelson, Ryan Keddy, Michael Tufano, Daniel D. Caspi, Preethi Krishnan, Neeta Mistry, Gennadiy Koev, Thomas J. Reisch, Rubina Mondal, Tami Pilot-Matias, Yi Gao, David W. A. Beno, Clarence J. Maring, Akhter Molla, Emily Dumas, Andrew Campbell, Laura Williams, Christine Collins, Rolf Wagner, and Warren M. Kati, Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A, J. Med. Chem., 2014, 57 (5), pp 2047–2057

http://dx.doi.org/10.1021/jm401398x

Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir, Br. J. Clin. Pharmacol., 1997, 44 (2), pp 190-194

http://dx.doi.org/10.1046%2Fj.1365-2125.1997.00644.x

http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206619lbl.pdf

[2014-Dec-19] FDA approves Lynparza to treat advanced ovarian cancer

http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm427554.htm

 Lynparza.cdx

Keith A. Menear, Claire Adcock, Robert Boulter, Xiao-ling Cockcroft, Louise Copsey, Aaron Cranston, Krystyna J. Dillon, Jan Drzewiecki, Sheila Garman, Sylvie Gomez, Hashim Javaid, Frank Kerrigan, Charlotte Knights, Alan Lau, Vincent M. Loh , Jr., Ian T. W. Matthews, Stephen Moore, Mark J. O’Connor, Graeme C. M. Smith and Niall M. B. Martin, 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1, J. Med. Chem., 2008, 51 (20), pp 6581–6591

http://dx.doi.org/10.1021/jm8001263

Valérie Schreiber, Françoise Dantzer, Jean-Christophe Ame and Gilbert de Murcia, Poly(ADP-ribose): novel functions for an old molecule, Nat. Rev. Mol. Cell Biol., 2006, 7 (7), pp 517-528

http://dx.doi.org/10.1038/nrm1963

Prakash Jagtap and Csaba Szabó, Poly(ADP-ribose) polymerase and the therapeutic effects of its inhibitors, Nat. Rev. Drug Discov., 2005, 4 (5), 421-440

http://dx.doi.org/10.1038/nrd1718

[2014-Oct-29] US FDA approves once-daily XIGDUO™ XR tablets for adults with Type 2 Diabetes

http://www.astrazeneca.com/Media/Press-releases/Article/20141030-us-fda-approve-oncedaily-xigduo-xr

xigduo.cdx

[1994-Dec-30] Metformin

http://web.archive.org/web/20070929152824/http://www.fda.gov/bbs/topics/ANSWERS/ANS00627.html

 Metformin.cdx

T94-64                                            Susan M. Cruzan
Dec. 30, 1994                                     301-443-3285

                 FDA APPROVES NEW DIABETES DRUG

     We have been receiving inquiries about the approval of metformin, a new drug for treatment of adult onset non-insulin dependent, or type II, diabetes, a serious disorder of blood sugar control.  Type II diabetes afflicts 12 million Americans and can cause damage to the eyes, kidneys, heart and peripheral circulation.  The following may be useful in answering questions. 
     Patients with type II diabetes are generally advised to lose weight and maintain a strict diet.  If these measures fail to control blood sugar levels, they are generally prescribed oral drugs and, if these fail, insulin injections.  
     Metformin is an oral medication for controlling elevated blood sugar levels in type II diabetes.  It differs from other currently approved antidiabetic drugs chemically and in how it works.  It can be used together with currently available oral antidiabetic drugs.  
     In March 1994, an FDA advisory committee voted unanimously to recommend that FDA approve metformin for people with diabetes who cannot achieve adequate blood sugar control with diet alone. At this meeting the president of the American Diabetes Association urged approval of metformin as a safe and effective drug that controls blood glucose by mechanisms different from currently available drugs.  
     In people with diabetes, the pancreas does not produce enough insulin to control blood sugar, which then rises to harmful levels.  Metformin and other oral anti-diabetic drugs lower these elevated blood sugar levels.  Currently approved and marketed anti-diabetic drugs work by stimulating the pancreas to secrete more insulin.  Metformin increases the body's response to its own insulin.  Unlike the other drugs, metformin rarely causes hypoglycemia and generally does not cause weight gain.  It may cause temporary anorexia (loss of appetite), abdominal discomfort or nausea.
     One concern with oral antidiabetic drugs -- including metformin -- is the potential risk of cardiovascular death.  A warning to this effect is contained in the labeling for these drugs.  Studies are under way to gain more information about this and other complications.
     Safety concerns about a related drug -- phenformin -- resulted in its being removed from the market in 1977. Phenformin was found to promote the development of lactic acidosis, a life-threatening buildup of lactic acid in the blood that was fatal in about one patient in one thousand treated for a year.  Numerous studies with metformin and marketing experience in other countries have shown that, although it can cause lactic acidosis, the risk is much less than that of phenformin.
     Patients given metformin should be made aware of lactic acidosis symptoms -- malaise, rapid breathing, shortness of breath and severe weakness  -- and be advised to contact their doctors immediately if they experience any of these.  Lactic acidosis can be diagnosed with laboratory tests and requires that metformin therapy be stopped immediately and proper supportive care initiated. 
     During worldwide marketing, patients on metformin have developed lactic acidosis at about one tenth the rate of those on phenformin.   Metformin has been approved in about 80 countries and has never been withdrawn for safety reasons.  The manufacturer, Lipha Pharmaceuticals Co. of New York, N.Y., submitted an application for marketing to FDA in September l993.  
      A patient package insert will be included with metformin. 
Lipha will conduct an educational campaign to inform health professionals and patients about the drug's risks and benefits and appropriate precautions.  The company will also conduct a postmarketing study in 10,000 patients to increase knowledge about potential safety problems.
      Metformin will be sold under the trade name Glucophage. The product will be distributed in the United States by Bristol-Myers Squibb of Princeton, N.J.