Uterine fibroids are benign hormone-sensitive tumors of uterine smooth muscle cells leading to heavy menstrual bleeding and pelvic pain. Ulipristal acetate (UPA) is an emerging medical treatment of fibroids with the potential to be used for long-term treatment. In this context, the present article summarizes UPA’s main clinical pharmacology and pharmacokinetic (PK) properties. Ulipristal acetate has good oral bioavailability and a half-life allowing one single oral administration per day for the management of fibroids. As a steroid, UPA is a substrate for cytochrome P450 (CYP) 3A4 but does not act as an inducer or inhibitor of the CYP system or transporter proteins. With the exception of drugs modulating CYP3A4 activity, risks of drug-drug interactions with UPA are unlikely. In conclusion, besides its pharmacodynamic characteristics, UPA shows favorable PK properties that contribute to a good efficacy-safety ratio for the long-term management of uterine fibroids in clinical practice.
© The Author(s) 2014.

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On March 30, 2016 Amal Therapeutics (Amal) reported that they have completed CHF 3 million (EUR 2.75 million) Series A financing round with Boehringer Ingelheim Venture Fund (BIVF) as cornerstone investors (Press release, Boehringer Ingelheim, MAR 29, 2016, View Source [SID:1234510134]). VI Partners and High-Tech Gründerfonds also participated in the round which will help progress Amal’s cancer vaccines.

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Amal Therapeutics is a Swiss biotech company developing and progressing therapeutic cancer vaccines. The company will use the funds to progress the preclinical development of its lead vaccine (ATP124) for colorectal cancer and to further develop its KISIMA technology platform for therapeutic tumor vaccination. This novel technology is able to generate potent long lasting anti-tumor immunity and avoid tumor immune escape.

Dr. Frank Kalkbrenner from the Boehringer Ingelheim Venture Fund and Dr. Frank Hensel from the High-Tech Gruenderfonds will join the Board as Board Observers. Dr. Diego Braguglia from VI Partners will also become a member of Amal’s Supervisory Board.

Dr. Madiha Derouazi, CEO and founder of Amal Therapeutics said: "This Series A investment recognizes the potential of the KISIMA technology platform and the value of our scientific assets. We are now in a position to rapidly progress our lead vaccine, ATP124, for colorectal cancer into the clinic and continue to develop our pipeline in other cancer indications. I look forward to working with the Board to make Amal Therapeutics a leading innovator in the field of immunotherapies".

Dr. Knut Elbers, Boehringer Ingelheim Venture Fund representative on Amal’s Board added: "Dr. Derouazi’s dedicated leadership and scientific expertise allowed us to assemble a group of outstanding scientists to show proof-of-principle in a series of pre-clinical tumor studies. We are confident that Amal’s KISIMA technology could revolutionize the peptide-based cancer vaccine field – bringing an exciting new technology to the patient".

Dr. Braguglia, VI Partners: "We believe that the KISIMA technology is superior to many other tumor vaccine technologies, both as a stand-alone treatment and in combination with other vaccines or immuno-oncology treatment modalities. I’m pleased to be joining the current seasoned investors and support the team of Amal in moving its technology into the clinic".

Amal’s vaccines combine a Cell Penetrating Peptide (CPP) with a multi-antigenic chimeric cargo with various CD8+ and CD4+ epitopes and a constitutive activator of dendritic cells, enabling them to simultaneously stimulate multi-epitopic cytotoxic T cell-mediated immunity, induce helper T (Th) cells and promote immunological memory.

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Chronic hepatitis B infection (CHB) is characterized by sub-optimal T cell responses to viral antigens. A therapeutic vaccine capable of restoring these immune responses could potentially improve HBsAg seroconversion rates in the setting of direct acting antiviral therapies. A yeast-based immunotherapy (Tarmogen) platform was used to make a vaccine candidate expressing hepatitis B virus (HBV) X, surface (S), and Core antigens (X-S-Core). Murine and human immunogenicity models were used to evaluate the type and magnitude of HBV-Ag specific T cell responses elicited by the vaccine. C57BL/6J, BALB/c, and HLA-A*0201 transgenic mice immunized with yeast expressing X-S-Core showed T cell responses to X, S and Core when evaluated by lymphocyte proliferation assay, ELISpot, intracellular cytokine staining (ICS), or tumor challenge assays. Both CD4+ and CD8+ T cell responses were observed. Human T cells transduced with HBc18-27 and HBs183-91 specific T cell receptors (TCRs) produced interferon gamma (IFNγ following incubation with X-S-Core-pulsed dendritic cells (DCs). Furthermore, stimulation of peripheral blood mononuclear cells (PBMCs) isolated from CHB patients or from HBV vaccine recipients with autologous DCs pulsed with X-S-Core or a related product (S-Core) resulted in pronounced expansions of HBV Ag-specific T cells possessing a cytolytic phenotype. These data indicate that X-S-Core-expressing yeast elicit functional adaptive immune responses and supports the ongoing evaluation of this therapeutic vaccine in patients with CHB to enhance the induction of HBV-specific T cell responses.

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(Filing, Annual, AEterna Zentaris, 2015, MAR 29, 2016, View Source [SID:1234510132])

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Glucose transporters are central players in glucose homeostasis. There are two major classes of glucose transporters in the body, the passive (GLUTs) and the secondary active or sodium-coupled transporters (SGLTs). Here we report the use of a non-invasive imaging technique, Positron Emission Tomography (PET) in mice, to evaluate the role of GLUTs and SGLTs in controlling glucose distribution and utilization. We show that GLUTs are most significant for glucose in uptake into the brain and liver while SGLTs are important in glucose recovery in the kidney. This work provides further support to the use of SGLT imaging to study the role of SGLT transporters in human physiology and diseases such as diabetes and cancer.
The importance of SGLTs and GLUT2 in glucose homeostasis was studied in mice using fluorine-18 labelled glucose molecular imaging probes and non-invasive PET imaging. The probes were: Me-4FDG, a substrate for SGLTs; 4-FDG, a substrate for SGLTs and GLUTs; and 2-FDG, a substrate for GLUTs. These radiolabelled imaging probes were injected intravenously into wild-type, Sglt1(-/-) , Sglt2(-/-) and Glut2(-/-) mice and their dynamic whole-body distribution was determined using microPET. The distribution of 2-FDG was similar to that reported earlier, i.e. it accumulated in brain, heart, liver, and kidney and was excreted into the urinary bladder. There were little changes in 2-FDG distribution in Glut2(-/-) mice apart from a reduction in the rate of uptake into liver. The major differences between Me-4FDG and 2-FDG were that Me-4FDG did not enter the brain and was not excreted into the urinary bladder. There was urinary excretion of Me-4FDG in Sglt1(-/-) and Sglt2(-/-) mice. However, Me-4FDG was not reabsorbed in the kidney in Glut2(-/-) mice. There were no differences in Me-4FDG uptakes into heart of wild-type, Sglt1(-/-) and Sglt2(-/-) mice. We conclude that GLUT2 is important in glucose liver transport and reabsorption of glucose in the kidney along with SGLT2 and SGLT1. Complete reabsorption of Me-4FDG from the glomerular filtrate in wild-type mice and the absence of reabsorption in the kidney in Glut2(-/-) mice confirm the importance of GLUT2 in glucose absorption across the proximal tubule. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.

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