Utilisation of the Innovative [18F]-Labelled Radiotracer [18F]-BIBD-071 Within HR+ Breast Cancer Xenograft Mouse Models by Di Fan, Xin Wang, Xueyuan Ling, Hongbin Li, Lu Zhang, Wei Zheng, Zehui Wu, Lin Ai

“…<b>Background/Objectives:</b> Aromatase plays a crucial role in the conversion of androgens to oestrogens and is often overexpressed in hormone-dependent tumours, particularly breast cancer. [18F]BIBD-071, which has excellent binding affinity for aromatase and good pharmacokinetics, has potential for the diagnosis and treatment of aromatase-related diseases. …”
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Clinical trial to compare safety and tolerability between intravenous infusion and bolus intravenous injection of ApTOLL in healthy volunteers by Macarena Hernández-Jiménez, Samuel Martín-Vílchez, Gina Mejía-Abril, Manuel Roman, Sergio Luquero-Bueno, David Piñeiro, Marc Ribó, Francisco Abad-Santos, Dolores Ochoa

“…The objective was to assess the safety and pharmacokinetics of ApTOLL when comparing intravenous infusion (30 min) vs. bolus intravenous injection (1–3 min). …”
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Fermented sugarcane juice-derived probiotic Levilactobacillus brevis RAMULAB54 enhances lipid metabolism and glucose homeostasis through PPAR-γ activation by V. B. Chandana Kumari, Ramith Ramu, Sujay S. Huligere, Shashank M. Patil, Shivasharanappa Nayakvadi, Sharath Bijoor, Uma Venkateswaran Manjappara, Mohammad Z. Ahmed, Ling Shing Wong

“….−8.3 kcal/mol), with greater stability (RMSD: 1.2 Å vs. 1.7 Å). Pharmacokinetics indicated moderate GI absorption (20%) and low toxicity for hydroxycitric acid. …”
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Increasing brain half-life of antibodies by additional binding to myelin oligodendrocyte glycoprotein, a CNS specific protein by Marie-Lynn Cuypers, Tom Jaspers, Jarne Clerckx, Simon Leekens, Christopher Cawthorne, Guy Bormans, Frederik Cleeren, Nick Geukens, Bart De Strooper, Maarten Dewilde

“…Their ability to increase the brain half-life of antibodies was evaluated in healthy wild-type mice by coupling two different MOG VHHs (low/high affinity) in a mono- and bivalent format to a β-secretase 1 (BACE1) inhibiting antibody or a control (anti-SARS-CoV-2) antibody, fused to an anti-transferrin receptor (TfR) VHH for active transport over the BBB. Brain pharmacokinetics and pharmacodynamics, CNS and peripheral biodistribution, and brain toxicity were evaluated after intravenous administration to balb/c mice. …”
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Overview of preclinical and phase II clinical studies on Pegmolesatide’s long-term erythropoiesis stimulating effect via EPOR-mediated signal transduction by Xiaoying Ma, Zhen Li, Lu Zhang, Hui Qian, Qinkai Chen, Ye Tao, Yunfan Li, Dandan Wang, Zhizhen Hu, Weili Luo, Ping Li, Hai Yu, Changlin Mei, Xueqing Yu, Yuanfeng Zhou

“…Methods In vitro assays were utilized to assess Pegmolesatide erythropoietin receptor (EPOR) affinity, competitive binding, cell proliferation/survival, apoptosis, cell surface receptor expression, and signal transduction. Pharmacokinetics (PK) and Pharmacodynamics (PD) parameters were evaluated in BALB/c mice following single administration. …”
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Wound irrigation and peritoneal lavage with antiseptic/antibiotic solution before wound closure during gastrointestinal surgery: a systematic review and meta-analysis by Motoi Uchino, Koji Tamura, Shinsuke Nomura, Seiichi Shinji, Keita Kouzu, Hiroji Shinkawa, Tomohiro Ishinuki, Toru Mizuguchi, Hiroki Ohge, Seiji Haji, Junzo Shimizu, Yasuhiko Mohri, Chizuru Yamashita, Yuichi Kitagawa, Katsunori Suzuki, Motomu Kobayash, Masahiro Kobayashi, Yuki Hanai, Hiroshi Nobuhara, Hiroki Imaoka, Masahiro Yoshida, Toshihiko Mayumi, Hiroki Ikeuchi, on behalf of SSI Prevention Guideline Committee in Japan Society for Surgical Infection

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Impact of iron chelation with deferasirox on telomere length and oxidative stress in hemodialysis patients: A randomized study by Blanca Olivia Murillo Ortiz, Joel Ramírez Emiliano, Marcos Javier Romero Vázquez, Lauro Fabián Amador Medina, Sandra Martínez Garza, Edna Montserrat Ramos Rodríguez

“…To evaluate the pharmacokinetics and safety of deferasirox, plasma concentrations were analyzed by HPLC. …”
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Poor efficacy of the combination of clarithromycin, amikacin, and cefoxitin against Mycobacterium abscessus in the hollow fiber infection model by Etienne Vignaud, Sylvain Goutelle, Charlotte Genestet, Jérôme Guitton, Sabine Cohen, Chloé Bourg, Aurore Durand, Laura Lebouteiller, Albin Bernard, Caroline Richet, Oana Dumitrescu, Elisabeth Hodille

“…Two level of macrolide concentrations were evaluated mimicking the pharmacokinetics profiles of free (i.e. unbound) drug in blood and lung. …”
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Safety and tolerability of the M2 muscarinic acetylcholine receptor modulator BAY 2413555 in heart failure with reduced ejection fraction in the REMOTE-HF study by Marat Fudim, Muhammad Shahzeb Khan, Dominik Linz, JoAnn Lindenfeld, Calum MacRae, Nina Kimmeskamp-Kirschbaum, Michaela Meyer, Thomas Mondritzki, Hanna Tinel, Wilfried Dinh, Robert J. Mentz

“…This study tested the safety, tolerability and pharmacokinetics of this novel therapeutic option. REMOTE-HF was a multicenter, double-blind, randomized, placebo-controlled, phase Ib dose-titration study with two active arms. …”
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Sitravatinib in combination with nivolumab plus ipilimumab in patients with advanced clear cell renal cell carcinoma: a phase 1 trial by Pavlos Msaouel, Kai Yu, Ying Yuan, Jianfeng Chen, Xinmiao Yan, Menuka Karki, Fei Duan, Rahul A. Sheth, Priya Rao, Kanishka Sircar, Amishi Y. Shah, Amado J. Zurita, Giannicola Genovese, Min Li, Chih-Chen Yeh, Minghao Dang, Guangchun Han, Yanshuo Chu, Max Hallin, Peter Olson, Rui Yang, Daniela Slavin, Hirak Der-Torossian, Curtis D. Chin, Nizar M. Tannir, Linghua Wang, Jianjun Gao

“…Secondary endpoints were objective response rate (ORR), disease control rate (DCR), duration of response (DOR), progression-free survival (PFS), overall survival (OS), 1-year survival probability, and sitravatinib pharmacokinetics. Sitravatinib dose of 35 mg daily plus nivolumab 3 mg/kg and ipilimumab 1 mg/kg resulted in high frequency of immune-related adverse events. …”
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Safety and efficacy of trifluridine/tipiracil +/− bevacizumab plus XB2001 (anti-IL-1α antibody): a single-center phase 1 trial by Marion Thibaudin, Nicolas Roussot, Chloé Burlot, Antonin Schmitt, Julie Vincent, Zoé Tharin, Leila Bengrine, Hélène Bellio, Aurélie Bertaut, Léa Hampe, Susy Daumoine, Emilie Rederstorff, Morgane Peroz, Titouan Huppe, Valentin Derangère, David Rageot, John Simard, Caroline Truntzer, Jean David Fumet, Francois Ghiringhelli

“…Safety, efficacy, pharmacokinetics and pharmacodynamics were assessed. Seventeen patients (median age: 67.4 years) were enroled. …”
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Long-Term Therapeutic Effects of ²²⁵Ac-DOTA-E[c(RGDfK)]₂ Induced by Radiosensitization via G2/M Arrest in Pancreatic Ductal Adenocarcinoma by Mitsuyoshi Yoshimoto, Kohshin Washiyama, Kazunobu Ohnuki, Ayano Doi, Miki Inokuchi, Motohiro Kojima, Brian W. Miller, Yukie Yoshii, Anri Inaki, Hirofumi Fujii

“…²²⁵Ac-DOTA-RGD₂ (20, 40, 65, or 90 kBq) showed favorable pharmacokinetics and remarkable tumor growth inhibition without severe side effects in the BxPC-3 mouse model. …”
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Induced-volatolomics, a new research field in chemical biology by Blochouse, Estelle, Eid, Rony, Cannoni, Elsa, Châtre, Rémi, Geffroy, Claude, Opalinski, Isabelle, Papot, Sébastien, Poinot, Pauline

“…However, these imaging tools meet several bottlenecks related to either stability, background noise, limited penetration depth or systemic toxicity, pharmacokinetics, tissue distribution, and renal clearance.In parallel, novel volatile organic compound (VOC)-based probes have been proposed under the emerging paradigm of induced-volatolomics. …”
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Exploring the Potential of Malvidin and Echiodinin as Probable Antileishmanial Agents Through In Silico Analysis and In Vitro Efficacy by Luis Daniel Goyzueta-Mamani, Daniela Pagliara Lage, Haruna Luz Barazorda-Ccahuana, Margot Paco-Chipana, Mayron Antonio Candia-Puma, Gonzalo Davila-Del-Carpio, Alexsandro Sobreira Galdino, Ricardo Andrez Machado-de-Avila, Rodolfo Cordeiro Giunchetti, Edward L. D’Antonio, Eduardo Antonio Ferraz Coelho, Miguel Angel Chávez-Fumagalli

“…These findings suggest malvidin’s potential as a safe, natural antileishmanial compound, warranting further in vivo studies to confirm its therapeutic efficacy and pharmacokinetics in animal models.…”
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Impact of antibody architecture and paratope valency on effector functions of bispecific NKp30 x EGFR natural killer cell engagers by Ammelie Svea Boje, Lukas Pekar, Katharina Koep, Britta Lipinski, Brian Rabinovich, Andreas Evers, Carina Lynn Gehlert, Steffen Krohn, Yanping Xiao, Simon Krah, Rinat Zaynagetdinov, Lars Toleikis, Sven Poetzsch, Matthias Peipp, Stefan Zielonka, Katja Klausz

“…However, the fusion of sdAbs can have a slight impact on the NK cell release of immunomodulatory cytokines, as well as on the pharmacokinetic profile of the NKCE due to unfavorable spatial orientation within the molecule architecture. …”
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Impact of iron chelation with deferasirox on telomere length and oxidative stress in hemodialysis patients: A randomized study by Blanca Olivia Murillo Ortiz, Joel Ramírez Emiliano, Marcos Javier Romero Vázquez, Lauro Fabián Amador Medina, Sandra Martínez Garza, Edna Montserrat Ramos Rodríguez

“…To evaluate the pharmacokinetics and safety of deferasirox, plasma concentrations were analyzed by HPLC. …”
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GrB-Fc-KS49, an anti-EMP2 granzyme B fusion protein therapeutic alters immune cell infiltration and suppresses breast cancer growth by Ana Alvarez de Cienfuegos, Lawrence H Cheung, Khalid A Mohamedali, Michael G Rosenblum, Brian Aguirre, Cheng-Hsiang Lu, Anubhav Chandla, Nidhi Kejriwal, Lucia Liu, Ann M Chan, SuYin Kok, Sergio Duarte, David Casero, Madhuri Wadehra

“…The construct’s pharmacokinetics (PK), toxicity profile, and in vivo efficacy were also evaluated.Results GrB-Fc-KS49 exhibited comparable GrB enzymatic activity to commercial GrB, as well as high affinity to an EMP2 peptide, with the dissociation constant in the picomolar range. …”
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Dual inhibition of LAG-3 and PD-1 with IBI110 and sintilimab in advanced solid tumors: the first-in-human phase Ia/Ib study by Chenyu Mao, Anwen Xiong, Jiong Qian, Wenxiang Wang, Ying Liu, Tao Zhang, Zhihai Wu, Haiqing Ni, Jia Lu, Sixiang Long, Li Zhao, Yuling Chen, Caicun Zhou, Nong Xu

“…The secondary endpoints included pharmacokinetics, pharmacodynamics and immunogenicity. …”
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Local and distant response to intratumoral immunotherapy assessed by immunoPET in mice by Aurélien Marabelle, Louis Meyblum, Lambros Tselikas, Thierry de Baere, Sandrine Susini, Fréderic Deschamps, Baptiste Bonnet, Céline Chevaleyre, Benoit Jego, Dimitri Kereselidze, Vincent Lebon, Charles Truillet

“…Consistent intratumoral pharmacodynamic effects were observed in both intratumoral and intravenous treatment groups, as evidenced by a notable increase in CD8+T cells within the CT26 tumors following treatment.Conclusions ImmunoPET-derived pharmacokinetics supports intratumoral injection of ICBs to decrease systemic exposure while maintaining efficacy compared with intravenous. …”
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Real-World Evidence of Clinical Outcomes of the Use of the Adalimumab Biosimilar SB5 in Rheumatic and Gastrointestinal Immune-Mediated Inflammatory Diseases: 12-Month Data from the... by Bruno Fautrel, Yoram Bouhnik, Carine Salliot, Franck Carbonnel, Mathurin Fumery, Christophe Bernardeau, Yves Maugars, Mathurin Flamant, Fabienne Coury, Ben Braithwaite, Salima Hateb, Janet Addison, the PERFUSE investigators

“…Abstract Background There is a need for published data on real-world use of SB5, an adalimumab (ADL) biosimilar approved in Europe in 2017, on the basis of evidence from pre-clinical and analytic data as well as phase I and III clinical studies demonstrating equivalent efficacy and comparable pharmacokinetics, safety and immunogenicity profiles as the reference ADL. …”
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