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Patterns of genomic instability in > 2000 patients with ovarian cancer across six clinical trials evaluating olaparib.
Genome Med
December 2024
Translational Medicine, Oncology R&D, AstraZeneca, Cambridge Biomedical Campus, 1 Francis Crick Avenue, Cambridge, CB2 0AA, UK.
Background: The introduction of poly(ADP-ribose) polymerase (PARP) inhibitors represented a paradigm shift in the treatment of ovarian cancer. Genomic data from patients with high-grade ovarian cancer in six phase II/III trials involving the PARP inhibitor olaparib were analyzed to better understand patterns and potential causes of genomic instability.
Patients And Methods: Homologous recombination deficiency (HRD) was assessed in 2147 tumor samples from SOLO1, PAOLA-1, Study 19, SOLO2, OPINION, and LIGHT using next-generation sequencing technology.
Evaluation of Olaparib Tablet Safety and Pharmacokinetics in Healthy Chinese Male Subjects.
Drug Des Devel Ther
December 2024
Clinical Department, CSPC Zhongqi Pharmaceutical Technology (SJZ) Co., LTD., Shijiazhuang, Hebei Province, People's Republic of China.
Purpose: To evaluate the safety and pharmacokinetics of olaparib tablet test formulation (T) and reference formulation (R) in healthy Chinese male subjects.
Subjects And Methods: This was a single-dose, randomized-sequence, two-way crossover study including three parts: part A: a safety exploration design in lower dose (n = 14, 100 mg), part B: a pivotal comparative pharmacokinetic (PK) trial under fast condition (n = 44, 150 mg) and part C: a pivotal comparative PK trial under food condition (n = 44, 150 mg). Blood samples were collected for 72 hours and the PK parameters of C, AUC and AUC were used to evaluate PK differences.
Synthesis and Structure of Novel Hybrid Compounds Containing Phthalazin-1(2)-imine and 4,5-Dihydro-1-imidazole Cores and Their Sulfonyl Derivatives with Potential Biological Activities.
Int J Mol Sci
October 2024
Department of Chemical Technology of Drugs, Faculty of Pharmacy, Medical University of Gdansk, Gen. J. Hallera 107, 80-416 Gdańsk, Poland.
A novel hybrid compound-2-(4,5-dihydro-1-imidazol-2-yl)phthalazin-1(2)-imine () was synthesized and converted into di-substituted sulfonamide derivatives - and phthalazine ring opening products-hydrazonomethylbenzonitriles -. The newly prepared compounds were characterized using elemental analyses, IR and NMR spectroscopy, as well as mass spectrometry. Single crystal X-ray diffraction data were collected for the representative compounds , , , , and .
View Article and Find Full Text PDFDevelopment and Characterization of Olaparib-Loaded Solid Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) for Pharmaceutical Applications.
AAPS PharmSciTech
September 2024
Department of Global Innovative Drugs, The Graduate School of Chung-Ang University, 221 Heukseok-Dong, Dongjak-Gu, Seoul, 06974, Republic of Korea.
This study aims to enhance the solubility of Olaparib, classified as biopharmaceutical classification system (BCS) class IV due to its low solubility and bioavailability using a solid self-nanoemulsifying drug delivery system (S-SNEDDS). For this purpose, SNEDDS formulations were created using Capmul MCM as the oil, Tween 80 as the surfactant, and PEG 400 as the co-surfactant. The SNEDDS formulation containing olaparib (OLS-352), selected as the optimal formulation, showed a mean droplet size of 87.
View Article and Find Full Text PDFRecent synthetic strategies for the functionalization of fused bicyclic heteroaromatics using organo-Li, -Mg and -Zn reagents.
Chem Soc Rev
November 2024
Department of Chemistry, Ludwig-Maximilians-University München, Butenandtstrasse 5-13, Haus F, 81377 Munich, Germany.
This review highlights the use of functionalized organo-Li, -Mg and -Zn reagents for the construction and selective functionalization of 5- and 6-membered fused bicyclic heteroaromatics. Special attention is given to the discussion of advanced syntheses for the preparation of highly functionalized heteroaromatic scaffolds, including quinolines, naphthyridines, indoles, benzofurans, benzothiophenes, benzoxazoles, benzothiazoles, benzopyrimidines, anthranils, thienothiophenes, purine coumarins, chromones, quinolones and phthalazines and their fused heterocyclic derivatives. The organometallic reagents used for the desired functionalizations of these scaffolds are generally prepared using the following methods: (i) through directed selective metalation reactions (DoM), (ii) by means of halogen/metal exchange reactions, (iii) through oxidative metal insertions (Li, Mg, Zn), and (iv) by transmetalation reactions (organo-Li and Mg transmetalations with ZnCl or ZnO(Piv)).
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