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Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives
Molecules 2009, 14, 2306-2316; doi:10.3390/molecules14072306 OPEN ACCESS molecules ISSN 1420-3049 www.mdpi.com/journal/molecules Article Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives Cheng Hua Huang 1,3, Hsien-Shou Kuo 2, Jia-Wen Liu 3 and Yuh-Ling Lin 3,* 1 Cathay General Hospital, 280 Renai Rd. Sec.4, Taipei, Taiwan 2 Department of Biochemistry, Taipei Medical University, 250 Wu-Hsin St. Taipei, Taiwan 3 College of Medicine, Fu-Jen Catholic University, 510 Chung Cheng Rd., Hsin-Chuang, Taipei Hsien 24205, Taiwan * Author to whom correspondence should be addressed; E-mail: [email protected] Received: 30 April 2009; in revised form: 19 June 2009 / Accepted: 23 June 2009 / Published: 29 June 2009 Abstract: Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC50 value of 2.02 M, and also weak cytotoxic activity against SF cells with an LC50 value over 10 M for 24 hr treatment. -
California Proposition 65 Toxicity List
STATE OF CALIFORNIA ENVIRONMENTAL PROTECTION AGENCY OFFICE OF ENVIRONMENTAL HEALTH HAZARD ASSESSMENT SAFE DRINKING WATER AND TOXIC ENFORCEMENT ACT OF 1986 CHEMICALS KNOWN TO THE STATE TO CAUSE CANCER OR REPRODUCTIVE TOXICITY 4-Mar-05 The Safe Drinking Water and Toxic Enforcement Act of 1986 requires that the Governor revise and Chemical Type of Toxicity CAS No. Date Listed A-alpha-C (2-Amino-9H-pyrido[2,3-b]indole) cancer 26148685 1-Jan-90 Acetaldehyde cancer 75070 1-Apr-88 Acetamide cancer 60355 1-Jan-90 Acetazolamide developmental 59665 20-Aug-99 Acetochlor cancer 34256821 1-Jan-89 Acetohydroxamic acid developmental 546883 1-Apr-90 2-Acetylaminofluorene cancer 53963 1-Jul-87 Acifluorfen cancer 62476599 1-Jan-90 Acrylamide cancer 79061 1-Jan-90 Acrylonitrile cancer 107131 1-Jul-87 Actinomycin D cancer 50760 1-Oct-89 Actinomycin D developmental 50760 1-Oct-92 Adriamycin (Doxorubicin hydrochloride) cancer 23214928 1-Jul-87 AF-2;[2-(2-furyl)-3-(5-nitro-2-furyl)]acrylamide cancer 3688537 1-Jul-87 Aflatoxins cancer --- 1-Jan-88 Alachlor cancer 15972608 1-Jan-89 Alcoholic beverages, when associated with alcohol abuse cancer --- 1-Jul-88 Aldrin cancer 309002 1-Jul-88 All-trans retinoic acid developmental 302794 1-Jan-89 Allyl chloride Delisted October 29, 1999 cancer 107051 1-Jan-90 Alprazolam developmental 28981977 1-Jul-90 Altretamine developmental, male 645056 20-Aug-99 Amantadine hydrochloride developmental 665667 27-Feb-01 Amikacin sulfate developmental 39831555 1-Jul-90 2-Aminoanthraquinone cancer 117793 1-Oct-89 p -Aminoazobenzene cancer -
Solid Forms of Ortataxel Feste Formen Von Ortataxel Formes Solides D’Ortataxel
(19) & (11) EP 2 080 764 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 493/04 (2006.01) A61K 31/357 (2006.01) 22.08.2012 Bulletin 2012/34 A61P 35/00 (2006.01) (21) Application number: 08000904.6 (22) Date of filing: 18.01.2008 (54) Solid forms of ortataxel Feste Formen von Ortataxel Formes solides d’ortataxel (84) Designated Contracting States: (74) Representative: Minoja, Fabrizio AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Bianchetti Bracco Minoja S.r.l. HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT Via Plinio, 63 RO SE SI SK TR 20129 Milano (IT) Designated Extension States: AL BA MK RS (56) References cited: WO-A-01/02407 WO-A-02/44161 (43) Date of publication of application: WO-A-2007/078050 US-A1- 2007 212 394 22.07.2009 Bulletin 2009/30 US-B1- 7 232 916 (73) Proprietor: INDENA S.p.A. • HENNENFENT K L ET AL: "NOVEL 20139 Milano (IT) FORMULATIONS OF TAXANES: A REVIEW. OLD WINE IN A NEW BOTTLE?" ANNALS OF (72) Inventors: ONCOLOGY,KLUWER, DORDRECHT, NL, vol. 17, • Ciceri, Daniele no. 5, 2006, pages 735-749, XP008065745 ISSN: 20139 Milano (IT) 0923-7534 • Sardone, Nicola • NICOLETTI MARIA INES ET AL: "IDN5109, a 20139 Milano (IT) taxane with oral bioavailability and potent • Gabetta, Bruno antitumor activity" CANCER RESEARCH, vol. 60, 20139 Milano (IT) no. 4, 15 February 2000 (2000-02-15), pages • Ricotti, Maurizio 842-846, XP002478136 ISSN: 0008-5472 20139 Milano (IT) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. -
Advances and Limitations of Antibody Drug Conjugates for Cancer
biomedicines Review Advances and Limitations of Antibody Drug Conjugates for Cancer Candice Maria Mckertish and Veysel Kayser * Sydney School of Pharmacy, Faculty of Medicine and Health, The University of Sydney, Sydney, NSW 2006, Australia; [email protected] * Correspondence: [email protected]; Tel.: +61-2-9351-3391 Abstract: The popularity of antibody drug conjugates (ADCs) has increased in recent years, mainly due to their unrivalled efficacy and specificity over chemotherapy agents. The success of the ADC is partly based on the stability and successful cleavage of selective linkers for the delivery of the payload. The current research focuses on overcoming intrinsic shortcomings that impact the successful devel- opment of ADCs. This review summarizes marketed and recently approved ADCs, compares the features of various linker designs and payloads commonly used for ADC conjugation, and outlines cancer specific ADCs that are currently in late-stage clinical trials for the treatment of cancer. In addition, it addresses the issues surrounding drug resistance and strategies to overcome resistance, the impact of a narrow therapeutic index on treatment outcomes, the impact of drug–antibody ratio (DAR) and hydrophobicity on ADC clearance and protein aggregation. Keywords: antibody drug conjugates; drug resistance; linkers; payloads; therapeutic index; target specific; ADC clearance; protein aggregation Citation: Mckertish, C.M.; Kayser, V. Advances and Limitations of Antibody Drug Conjugates for 1. Introduction Cancer. Biomedicines 2021, 9, 872. Conventional cancer therapy often entails a low therapeutic window and non-specificity https://doi.org/10.3390/ of chemotherapeutic agents that consequently affects normal cells with high mitotic rates biomedicines9080872 and provokes an array of adverse effects, and in some cases leads to drug resistance [1]. -
Research in Your Backyard Developing Cures, Creating Jobs
Research in Your Backyard Developing Cures, Creating Jobs PHARMACEUTICAL CLINICAL TRIALS IN ILLINOIS Dots show locations of clinical trials in the state. Executive Summary This report shows that biopharmaceutical research com- Quite often, biopharmaceutical companies hire local panies continue to be vitally important to the economy research institutions to conduct the tests and in Illinois, and patient health in Illinois, despite the recession. they help to bolster local economies in communities all over the state, including Chicago, Decatur, Joliet, Peoria, At a time when the state still faces significant economic Quincy, Rock Island, Rockford and Springfield. challenges, biopharmaceutical research companies are conducting or have conducted more than 4,300 clinical For patients, the trials offer another potential therapeutic trials of new medicines in collaboration with the state’s option. Clinical tests may provide a new avenue of care for clinical research centers, university medical schools and some chronic disease sufferers who are still searching for hospitals. Of the more than 4,300 clinical trials, 2,334 the medicines that are best for them. More than 470 of the target or have targeted the nation’s six most debilitating trials underway in Illinois are still recruiting patients. chronic diseases—asthma, cancer, diabetes, heart dis- ease, mental illnesses and stroke. Participants in clinical trials can: What are Clinical Trials? • Play an active role in their health care. • Gain access to new research treatments before they In the development of new medicines, clinical trials are are widely available. conducted to prove therapeutic safety and effectiveness and compile the evidence needed for the Food and Drug • Obtain expert medical care at leading health care Administration to approve treatments. -
Synthesis of 4-Hydroperoxy Derivatives of Ifosfamide and Trofosfamide by Direct Ozonation and Preliminary Antitumor Evaluation in V/Vo
[CANCER RESEARCH, 36, 2278-2281, July 1976] Synthesis of 4-Hydroperoxy Derivatives of Ifosfamide and Trofosfamide by Direct Ozonation and Preliminary Antitumor Evaluation in V/vo Hans-J. Hohorst, Gernot Peter, and Robert F. Struck Gustav-Embden-Zentrum der Biologischen Chemie, Abteilung KIr Zellchemie der J. W. Goethe-Universit~t, 6000 Frankfurt am Main, West Germany [H-J. H., G. P.], and Kettering-Meyer Laboratory, Southern Research Institute, Birmingham, Alabama 35205 [R. F. S.] SUMMARY reported routes (15, 17 to 19, 20), as well as to improve the yields. Two of us (11) have recently described such a syn- A one-step synthesis of 4-hydroperoxyifosfamide and 4- thesis of 4-hydroperoxycyclophosphamide, and application hydroperoxytrofosfamide is described. The method in- of this method to ifosfamide and trofosfamide and evalua- volves direct ozonation of ifosfamide and trofosfamide and tion of the products against leukemia L1210 in vivo are the offers improved yields in comparison with Fenton oxidation subjects of this report. The method is advantageous be- and greater convenience in comparison with ozonation of cause of its simplicity, its use of available starting materials, the appropriate 3-butenyl phosphorodiamidate. Evaluation the ease of isolation of products, and respectable yields. of the 4-hydroperoxy derivatives of cyclophosphamide, ifos- famide, and trofosfamide against leukemia L1210 in vivo suggests a superior effect for the ifosfamide derivative. MATERIALS AND METHODS Starting Materials. Cyclophosphamide, ifosfamide, and INTRODUCTION trofosfamide were obtained from Dr. Robert R. Engle, Drug Development Branch, National Cancer Institute, Silver Cyclophosphamide and its congeners ifosfamide and tro- Spring, Md., and from Asta Werke, 4800 Bielefeld, West fosfamide (1, 3) (Chart 1) are effective antitumor agents in Germany. -
SPECTRUM PHARMACEUTICALS, INC. (Exact Name of Registrant As Specified in Its Charter)
Table of Contents UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 FORM 8-K CURRENT REPORT PURSUANT TO SECTION 13 OR 15(D) OF THE SECURITIES AND EXCHANGE ACT OF 1934 Date of Report: July 20, 2007 SPECTRUM PHARMACEUTICALS, INC. (Exact name of registrant as specified in its charter) Delaware 000-28782 93-0979187 (State or other Jurisdiction (Commission File Number) (IRS Employer of Incorporation) Identification Number) 157 Technology Drive Irvine, California 92618 (Address of principal (Zip Code) executive offices) (949) 788-6700 (Registrant’s telephone number, including area code) N/A (Former Name or Former Address, if Changed Since Last Report) Check the appropriate box below if the Form 8-K filing is intended to simultaneously satisfy the filing obligation of the registrant under any of the following provisions: o Written communications pursuant to Rule 425 under the Securities Act (17 CFR 230.425) o Soliciting material pursuant to Rule 14a-12 under the Exchange Act (17 CFR 240.14a-12) o Pre-commencement communications pursuant to Rule 14d-2(b) under the Exchange Act (17 CFR 240.14d-2(b)) o Pre-commencement communications pursuant to Rule 13e-4(c) under the Exchange Act (17 CFR 240.13e-4(c)) TABLE OF CONTENTS Item 1.01 Entry Into Material Definitive Agreement. Item 8.01 Other Events. Item 9.01 Financial Statements and Exhibits. SIGNATURES EXHIBIT INDEX EXHIBIT 99.1 EXHIBIT 99.2 Table of Contents Item 1.01 Entry Into Material Definitive Agreement. On July 20, 2007, Spectrum Pharmaceuticals, Inc. (the “Company”) entered into a world-wide license agreement (the “License Agreement”) with Indena S.p.A., a Italian company (“Indena”), for ortataxel, a third-generation taxane classified as a new chemical entity that has demonstrated clinical activity in taxane-refractory tumors, effective as of July 17, 2007. -
Multicenter, Single Arm, Phase II Trial on the Efficacy of Ortataxel in Recurrent Glioblastoma (2019) Journal of Neuro-Oncology, 142 (3), Pp
Documents Export Date: 21 Jan 2020 Search: AU-ID("Gaviani, Paola" 6506528764) 1) Silvani, A., De Simone, I., Fregoni, V., Biagioli, E., Marchioni, E., Caroli, M., Salmaggi, A., Pace, A., Torri, V., Gaviani, P., Quaquarini, E., Simonetti, G., Rulli, E., D’Incalci, M., Poli, D., Mariotti, E., Caramia, G., Gritti, A.P., Pacchetti, I., Zucchetti, M., Lanza, A., Basso, G., Bini, P., Berzero, G., Diamanti, L., Di Cristofori, A., Manzoni, A., Lanfranchi, G., Ardizzoia, A., Villani, V. Multicenter, single arm, phase II trial on the efficacy of ortataxel in recurrent glioblastoma (2019) Journal of Neuro-Oncology, 142 (3), pp. 455-462. 1) https://www.scopus.com/inward/record.uri?eid=2-s2.0-85061248819&doi=10.1007%2fs11060-019-03116-z&partnerID=40&md5=55ca05a12a766ded77ba791fd16b7b7c DOI: 10.1007/s11060-019-03116-z Document Type: Article Publication Stage: Final Source: Scopus 2) Simonetti, G., Sommariva, A., Lusignani, M., Anghileri, E., Ricci, C.B., Eoli, M., Fittipaldo, A.V., Gaviani, P., Moreschi, C., Togni, S., Tramacere, I., Silvani, A. Prospective observational study on the complications and tolerability of a peripherally inserted central catheter (PICC) in neuro-oncological patients (2019) Supportive Care in Cancer, . 2) https://www.scopus.com/inward/record.uri?eid=2-s2.0-85075206792&doi=10.1007%2fs00520-019-05128-x&partnerID=40&md5=5550a094872f579fb7bf84be2a261c33 DOI: 10.1007/s00520-019-05128-x Document Type: Article Publication Stage: Article in Press Source: Scopus 3) Simonetti, G., Terreni, M.R., DiMeco, F., Fariselli, L., Gaviani, P. Letter to the editor: lung metastasis in WHO grade I meningioma (2018) Neurological Sciences, 39 (10), pp. -
Tanibirumab (CUI C3490677) Add to Cart
5/17/2018 NCI Metathesaurus Contains Exact Match Begins With Name Code Property Relationship Source ALL Advanced Search NCIm Version: 201706 Version 2.8 (using LexEVS 6.5) Home | NCIt Hierarchy | Sources | Help Suggest changes to this concept Tanibirumab (CUI C3490677) Add to Cart Table of Contents Terms & Properties Synonym Details Relationships By Source Terms & Properties Concept Unique Identifier (CUI): C3490677 NCI Thesaurus Code: C102877 (see NCI Thesaurus info) Semantic Type: Immunologic Factor Semantic Type: Amino Acid, Peptide, or Protein Semantic Type: Pharmacologic Substance NCIt Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells, while VEGF is overexpressed in many tumors and is correlated to tumor progression. PDQ Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor -
Functional Genomics Approaches to Elucidate Vulnerabilities of Intrinsic and Acquired Chemotherapy Resistance
cells Review Functional Genomics Approaches to Elucidate Vulnerabilities of Intrinsic and Acquired Chemotherapy Resistance Ronay Cetin 1,† , Eva Quandt 2,† and Manuel Kaulich 1,3,4,* 1 Institute of Biochemistry II, Goethe University Frankfurt-Medical Faculty, University Hospital, 60590 Frankfurt am Main, Germany; [email protected] 2 Faculty of Medicine and Health Sciences, Universitat Internacional de Catalunya, 08195 Barcelona, Spain; [email protected] 3 Frankfurt Cancer Institute, 60596 Frankfurt am Main, Germany 4 Cardio-Pulmonary Institute, 60590 Frankfurt am Main, Germany * Correspondence: [email protected]; Tel.: +49-(0)-69-6301-5450 † These authors contributed equally to this work. Abstract: Drug resistance is a commonly unavoidable consequence of cancer treatment that results in therapy failure and disease relapse. Intrinsic (pre-existing) or acquired resistance mechanisms can be drug-specific or be applicable to multiple drugs, resulting in multidrug resistance. The presence of drug resistance is, however, tightly coupled to changes in cellular homeostasis, which can lead to resistance-coupled vulnerabilities. Unbiased gene perturbations through RNAi and CRISPR technologies are invaluable tools to establish genotype-to-phenotype relationships at the genome scale. Moreover, their application to cancer cell lines can uncover new vulnerabilities that are associated with resistance mechanisms. Here, we discuss targeted and unbiased RNAi and CRISPR efforts in the discovery of drug resistance mechanisms by focusing on first-in-line chemotherapy and their enforced vulnerabilities, and we present a view forward on which measures should be taken to accelerate their clinical translation. Citation: Cetin, R.; Quandt, E.; Kaulich, M. Functional Genomics Keywords: chemotherapy resistance; cancer and drug vulnerabilities; functional genomics; RNAi Approaches to Elucidate Vulnerabilities of Intrinsic and and CRISPR screens Acquired Chemotherapy Resistance. -
Combination Effects of Radiotherapy / Drug Treatments for Cancer Recommendation by the German Commission on Radiological Protection with Scientific Background
Strahlenschutzkommission Geschäftsstelle der Strahlenschutzkommission Postfach 12 06 29 D-53048 Bonn http://www.ssk.de + Combination Effects of Radiotherapy / Drug Treatments for Cancer Recommendation by the German Commission on Radiological Protection with scientific Background Adopted at the 264th session of the SSK on 21 October 2013 Combination Effects of Radiotherapy / Drug Treatments for Cancer 2 The German original of this English translation was published in 2013 by the Federal Ministry for the Environment, Nature Conservation, Building and Nuclear Safety under the title: Kombinationswirkungen Strahlentherapie/medikamentöse Tumortherapie Empfehlung der Strahlenschutzkommission mit wissenschaftlicher Begründung This translation is for informational purposes only, and is not a substitute for the official statement. The original version of the statement, published on www.ssk.de, is the only definitive and official version. Combination Effects of Radiotherapy / Drug Treatments for Cancer 3 Contents Preface ....................................................................................................................... 8 Recommendation ...................................................................................................... 9 Scientific background of the recommendation .................................................... 11 1 Introduction ..................................................................................................... 11 2 Drug licensing and pharmacovigilance ....................................................... -
Chemotherapy for Metastatic Breast Cancer (MBC)
Clinical Conversations Between an Oncology Nurse and Oncology Pharmacist During the Treatment of Patients With Breast Cancer: A Focus on Oral Chemotherapeutic Formulations © 2020. All rights reserved. No part of this report may be reproduced or distributed without the expressed written permission of PTCE. Faculty Information Chair Danielle Roman, PharmD, BCOP Manager, Clinical Pharmacy Services Allegheny Health Network Pittsburgh, Pennsylvania Allison Butts, PharmD, BCOP Kandra Horne, DNP, APRN, WHNP-BC Clinical Coordinator, Oncology Pharmacy Women’s Health Care Nurse Practitioner UK HealthCare Breast and GYN Oncology: Medical Oncology Assistant Adjunct Professor Winship Cancer Institute: Emory Healthcare UK College of Pharmacy Atlanta, Georgia Lexington, Kentucky This activity is supported by an educational grant from Athenex. Educational Objectives At the completion of this activity, participants will be able to: • Distinguish optimized treatment approaches for breast cancer based on disease- and patient-specific factors and potential places in therapy for oral formulations • Analyze the results of recent clinical trials with recently approved and emerging treatment options to inform the appropriate management of adverse effects and adherence for patients with breast cancer • Examine the benefits of multidisciplinary care across multiple practice environments for patients with breast cancer to optimize patient outcomes Evolving Oral Chemotherapeutic Opportunities in Breast Cancer Care Danielle Roman, PharmD, BCOP Manager, Clinical Pharmacy