Background: The new generation anti-androgen enzalutamide and the potent CYP17 inhibitor abiraterone have both demonstrated survival benefits in patients with metastatic castration-resistant prostate cancer (CRPC) progressing after docetaxel. Preliminary data on the antitumour activity of abiraterone after enzalutamide have suggested limited activity. The antitumour activity and safety of enzalutamide after abiraterone in metastatic CRPC patients is still unknown.
Patients And Methods: We retrospectively identified patients treated with docetaxel and abiraterone prior to enzalutamide to investigate the activity and safety of enzalutamide in a more advanced setting. Prostate specific antigen (PSA), radiological and clinical assessments were analysed.
Results: 39 patients with metastatic CRPC were identified for this analysis (median age 70years, range: 54-85years). Overall 16 patients (41%) had a confirmed PSA decline of at least 30%. Confirmed PSA declines of ⩾50% and ⩾90% were achieved in 5/39 (12.8%) and 1/39 (2.5%) respectively. Of the 15 patients who responded to abiraterone, two (13.3%) also had a confirmed ⩾50% PSA decline on subsequent enzalutamide. Among the 22 abiraterone-refractory patients, two (9%) achieved a confirmed ⩾50% PSA decline on enzalutamide.
Conclusion: Our preliminary case series data suggest limited activity of enzalutamide in the post-docetaxel and post-abiraterone patient population.
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http://dx.doi.org/10.1016/j.ejca.2013.08.020 | DOI Listing |
Bioorg Med Chem Lett
January 2025
School of Cancer & Pharmaceutical Sciences, Faculty of Life Sciences & Medicine, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK. Electronic address:
The pyrrolobenzodiazepines (PBDs) represent a major class of sequence-selective DNA-alkylating molecules, one example of which, in its dimeric DNA-cross-linking form, is employed as the payload in the anticancer Antibody Drug Conjugate (ADC) loncastuximab tesirine-lpyl. To date, PBD analogues have been produced with substituents at every position of the tricyclic skeleton except the C1-position. We report here the first synthesis of a C1-subsitituted PBD monomer and dimer, both of which possess DNA-binding activity and cytotoxicity in a cancer cell line.
View Article and Find Full Text PDFPharmaceutics
December 2024
College of Pharmacy, Xinjiang Second Medical College, Karamay 834000, China.
, an active component of Arnebia euchroma (Royle) Johnst., has remarkable pharmacological effects, particularly in its anti-tumour activity. Nonetheless, the specific targets and mechanisms of action remain to be further explored.
View Article and Find Full Text PDFBiomolecules
November 2024
Department of Clinical and Experimental Medicine, University of Foggia, Via Rovelli 50, 71122 Foggia, Italy.
a South American ant species from the Formicidae family (subfamily Myrmicinae), has recently established a stable settlement in Europe, raising public health concerns due to its venomous stings. The venom of is rich in bioactive molecules, particularly piperidine alkaloids such as solenopsin A and peptides (Sol 1-4). These compounds have been implicated in various health applications, including antimicrobial, anti-inflammatory, and antitumour activities.
View Article and Find Full Text PDFCancers (Basel)
December 2024
Department of Cancer Immunotherapy, Fukuoka General Cancer Clinic, Fukuoka 812-0018, Japan.
: Neoantigens have attracted attention as ideal therapeutic targets for anti-tumour immunotherapy because the T cells that respond to neoantigens are not affected by central immune tolerance. Recent findings have revealed that the activation of CD4-positive T cells plays a central role in antitumor immunity, and thus targeting human leukocyte antigen (HLA) class II-restricted neoantigens, which are targets of CD4-positive T cells, is of significance. However, there are very few detailed reports of neoantigen vaccine therapies that use an HLA class II-restricted long peptide.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College, Kuvempu University, Shivamogga, Karnataka, India. Electronic address:
Plant based medicine is gaining recognition as a complementary approach to conventional treatments. Plants contain lectins that bind to carbohydrates and exhibit various biological properties and being used in cancer treatment. In present investigation Cordia myxa fruit was chosen, screen for presence of lectin and explore its biological role.
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