- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Journal: Total Synthesis of an Epothilone Analogue based on the Amide?Triazole Bioisosterism. (Pubmed Central) - Jun 26, 2024
Exploiting the amide-triazole bioisosterism, in this work we report the synthesis of the first generation of epothilones lacking the macrolide or azalide structure, with the ester or amide linkage replaced by a triazole unit. Together with the synthesis of this new analogue, computational and biological evaluations have been performed too.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Halaven (eribulin mesylate) / Eisai
Biomarker, Enrollment change, Trial completion date, Trial termination, Trial primary completion date, Biopsy: Pharmacodynamic Biomarkers of Standard Anti-microtubule Drugs as Assessed by Early Tumor Biopsy (clinicaltrials.gov) - Jun 25, 2024
P=N/A, N=5, Terminated,
Together with the synthesis of this new analogue, computational and biological evaluations have been performed too. N=35 --> 5 | Trial completion date: Aug 2024 --> Feb 2024 | Recruiting --> Terminated | Trial primary completion date: Jun 2024 --> Feb 2024; slow accrual
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Journal: Ixabepilone related angiographically silent macular edema. (Pubmed Central) - May 3, 2024
Angiographically silent intraretinal cystoid changes may develop in association with the use of ixabepilone. Referral to an ophthalmologist should be considered for the patients experiencing visual complaints as ixabepilone cessation may lead to visual improvement and avoid unnecessary treatment.
- |||||||||| Trial completion date, Metastases: Paclitaxel, Carboplatin, and Bevacizumab or Paclitaxel, Carboplatin, and Temsirolimus or Ixabepilone, Carboplatin, and Bevacizumab in Treating Patients With Stage III, Stage IV, or Recurrent Endometrial Cancer (clinicaltrials.gov) - Apr 4, 2024
P2, N=349, Active, not recruiting,
- |||||||||| Journal, PARP Biomarker, PD(L)-1 Biomarker, IO biomarker: Transcriptomic correlates of cell cycle checkpoints with distinct prognosis, molecular characteristics, immunological regulation, and therapeutic response in colorectal adenocarcinoma. (Pubmed Central) - Dec 29, 2023
Eventually, the GDSC database analysis showed that lower CCC scores were likely to be more sensitive to 5-fluorouracil, bosutinib, gemcitabine, gefitinib, methotrexate, mitomycin C, and temozolomide, while patients with higher CCC score seemed to have a higher level of sensitivity to bortezomib and elesclomol. The novel CCC signature exhibited a good ability for prognosis prediction for COAD patients, and the CCC score was found to be highly correlated with molecular features, immune-related characteristics, and therapeutic responses, which would greatly promote clinical management and precision medicine for COAD.
- |||||||||| Enrollment open, Metastases: ORIENTA: Organoid-based Functional Precision Therapy for Advanced Breast Cancer (clinicaltrials.gov) - Dec 29, 2023
P2, N=252, Recruiting,
The novel CCC signature exhibited a good ability for prognosis prediction for COAD patients, and the CCC score was found to be highly correlated with molecular features, immune-related characteristics, and therapeutic responses, which would greatly promote clinical management and precision medicine for COAD. Not yet recruiting --> Recruiting
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Avastin (bevacizumab) / Roche
Trial completion, Trial completion date: Evaluation of Weekly Ixabepilone With or Without Biweekly Bevacizumab (clinicaltrials.gov) - Nov 20, 2023
P2, N=78, Completed,
Trial primary completion date: Nov 2023 --> Jun 2024 Active, not recruiting --> Completed | Trial completion date: Feb 2024 --> Dec 2022
- |||||||||| colchicine / Generic mfg.
Review, Journal: Indole derivatives targeting colchicine binding site as potential anticancer agents. (Pubmed Central) - Jul 22, 2023
The structure-activity relationship studies have revealed the crucial pharmacophoric features required for the potent and selective binding of indole derivatives to the CBS. The development of these compounds with improved efficacy and reduced toxicity could potentially lead to the development of novel and effective cancer therapies.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Tafinlar (dabrafenib) / Novartis
Review, Journal: Biologically active sulfur-containing polyamides as promising anticancer materials. (Pubmed Central) - May 14, 2023
It was clear that there was an enhancement in the anticancer activity for the synthesized polyamides owing to the presence of the thiazole moiety as well as sulfur linkage. According to the results of the 50% inhibitory concentration (IC50), the synthesized polymers were found to be more active against the MCF-7 cell line than the HCT cell line.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Halaven (eribulin mesylate) / Eisai
Biomarker, Trial completion date, Trial primary completion date, Biopsy: Pharmacodynamic Biomarkers of Standard Anti-microtubule Drugs as Assessed by Early Tumor Biopsy (clinicaltrials.gov) - May 12, 2023
P=N/A, N=35, Recruiting,
According to the results of the 50% inhibitory concentration (IC50), the synthesized polymers were found to be more active against the MCF-7 cell line than the HCT cell line. Trial completion date: Aug 2023 --> Aug 2024 | Trial primary completion date: Jun 2023 --> Jun 2024
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, epothilone D (BMS-241027) / BMS, utidelone (UTD1) / Beijing Biostar Technologies
Review, Journal: Epothilones as Natural Compounds for Novel Anticancer Drugs Development. (Pubmed Central) - Apr 13, 2023
In recent years innovative synthetic strategies resulted in the synthesis of new epothilone derivatives with improved activity against refractory tumors with better activities when compared to ixabepilone or taxol. These compounds together with specific delivery mechanisms could be developed in anti-cancer drugs.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, patupilone (EPO 906) / Novartis, epothilone D (BMS-241027) / BMS
Journal: Rehabilitation enhances epothilone-induced locomotor recovery after spinal cord injury. (Pubmed Central) - Feb 7, 2023
As a result, principal component analysis of gait showed the greatest improvement in the epothilone B plus rehabilitation group. Thus, these results support the combination of epothilone B with rehabilitation in a clinical setting.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm
Enrollment change, Trial withdrawal: PREDATOR: Neoadjuvant Gene Prediction for Breast Cancer (clinicaltrials.gov) - Jan 18, 2023
P2, N=0, Withdrawn,
Thus, these results support the combination of epothilone B with rehabilitation in a clinical setting. N=14 --> 0 | Terminated --> Withdrawn
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Avastin (bevacizumab) / Roche
Trial completion date: Evaluation of Weekly Ixabepilone With or Without Biweekly Bevacizumab (clinicaltrials.gov) - Jan 12, 2023
P2, N=78, Active, not recruiting,
N=14 --> 0 | Terminated --> Withdrawn Trial completion date: Feb 2028 --> Feb 2024
- |||||||||| Journal: Bacteria as a treasure house of secondary metabolites with anticancer potential. (Pubmed Central) - Nov 18, 2022
Furthermore, we have also discussed some of the major secondary metabolites that are currently in the clinical trials or which have demonstrated potent anticancer activity in preclinical models. Besides, we have elaborated on the application of metagenomics in drug discovery and briefly described about anticancer agents identified through the metagenomics approach.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Review, Journal: Chemotherapy-induced peripheral neuropathy in children and adolescent cancer patients. (Pubmed Central) - Nov 1, 2022
Herein, we aim to provide an understanding of CIPN in the pediatric population and focus on the 6 main substance groups that frequently cause CIPN, namely the vinca alkaloids (vincristine), platinum-based antineoplastics (cisplatin, carboplatin and oxaliplatin), taxanes (paclitaxel and docetaxel), epothilones (ixabepilone), proteasome inhibitors (bortezomib) and immunomodulatory drugs (thalidomide). We discuss the clinical manifestations, assessments and diagnostic tools, as well as risk factors, pathophysiological processes and current pharmacological and non-pharmacological approaches for the prevention and treatment of CIPN.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Journal: Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry. (Pubmed Central) - Oct 26, 2022
By including a cooperativity factor (α) for curve fitting of allosteric modulators, this probe also allowed quantification of binding (K ) of the microtubule destabilizers colchicine (K = 80 nM, α = 0.08), vinblastine (K = 7 nM, α = 0.18), and maytansine (K = 3 nM, α = 0.21). Screening of this assay against 1008 NCI diversity compounds identified NSC 93427 as a novel microtubule destabilizer (K = 485 nM, α = 0.02), illustrating the potential of this approach for drug discovery.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Synribo (omacetaxine mepesuccinate) / Stragen, Teva, Istodax (romidepsin) / Astellas, BMS
FDA event, Journal: Pharmacological Landscape of FDA-approved Anticancer Drugs Reveals Sensitivities to Ixabepilone, Romidepsin, Omacetaxine, and Carfilzomib in Aggressive Meningiomas. (Pubmed Central) - Oct 26, 2022
In summary, a large-scale drug screening provides a comprehensive insight into the anti-meningioma activities of FDA-approved drugs, and identified carfilzomib, omacetaxine, ixabepilone, and romidepsin as novel potent antineoplastic agents for the treatment of aggressive meningiomas. The most pronounced effects were observed with ixabepilone mandating for further clinical investigation.
- |||||||||| Vumon (teniposide) / BMS
Journal: Effective Cancer Management: Inimitable Role of Phytochemical Based Nano-Formulations. (Pubmed Central) - Sep 7, 2022
These models can be utilized as a valuable tool in better understanding acquired resistance to palbociclib. The present review highlights the phytochemical-based nanoformulations and its strategies in the development of novel systems of drug delivery such as nano-liposomes, functionalized nanoparticles (NPs), and polymer nano-conjugates, SNEDDS (Self nano emulsifying drug delivery system) as this review paper depicts, as well as their rewards over conventional systems of drug delivery, as evidenced by improved biological activity depicted in their in vitro and in vivo anticancer assays.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Trial completion date, Trial primary completion date, Metastases: Anti-tumor Effect of Ixabepilone in Metastatic Breast Cancer (mBC) Selected by the Ixabepilone DRP. (clinicaltrials.gov) - Aug 22, 2022
P2, N=60, Recruiting,
This research also demonstrates the promising possibility of employing deep learning to develop drugs from natural products for a wider range of disorders. Trial completion date: Mar 2023 --> Nov 2025 | Trial primary completion date: Jan 2023 --> Nov 2023
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Avastin (bevacizumab) / Roche
Trial completion, Metastases: CALGB 40502: Paclitaxel, Nab-paclitaxel, or Ixabepilone With or Without Bevacizumab in Treating Patients With Stage IIIC or Stage IV Breast Cancer (clinicaltrials.gov) - Aug 5, 2022
P3, N=799, Completed,
Trial completion date: Oct 2022 --> Mar 2023 | Trial primary completion date: Jul 2022 --> Jan 2023 Active, not recruiting --> Completed
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Avastin (bevacizumab) / Roche
Trial completion date, Trial primary completion date: Evaluation of Weekly Ixabepilone With or Without Biweekly Bevacizumab (clinicaltrials.gov) - Apr 14, 2022
P2, N=78, Active, not recruiting,
TUBB3 is not a predictive biomarker. Trial completion date: Feb 2027 --> Feb 2028 | Trial primary completion date: Feb 2022 --> Feb 2023
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap, Yondelis (trabectedin) / Otsuka, PharmaMar, Valeo Pharma
Preclinical, Review, Journal: Natural Kinase Inhibitors for the Treatment and Management of Endometrial/Uterine Cancer: Preclinical to Clinical Studies. (Pubmed Central) - Mar 11, 2022
Pharmaceutical regimens based on two natural compounds, trabectedin and ixabepilone, have been investigated in humans showing short and midterm efficacy as second-line treatments in phase II clinical trials. The purpose of this review is twofold: the authors first provide an overview of the involvement of kinases and kinase inhibitors in the pathogenesis and treatment of EC and then discuss the existing evidence about natural products' derived kinase inhibitors in the management of the disease and outline relevant future research.
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm
Trial completion date, Trial primary completion date: Ixabepilone in Treating Participants With Significant Residual Disease of HER2/Neu Negative Invasive Breast Cancer After Systemic Therapy (clinicaltrials.gov) - Mar 10, 2022
P2, N=116, Active, not recruiting,
The purpose of this review is twofold: the authors first provide an overview of the involvement of kinases and kinase inhibitors in the pathogenesis and treatment of EC and then discuss the existing evidence about natural products' derived kinase inhibitors in the management of the disease and outline relevant future research. Trial completion date: Dec 2022 --> Dec 2024 | Trial primary completion date: Dec 2022 --> Dec 2024
- |||||||||| Ixempra (ixabepilone) - Otsuka, R / Pharm, Allarity Therap
Biomarker, Clinical, Journal: Systems pharmacogenomics identifies novel targets and clinically actionable therapeutics for medulloblastoma. (Pubmed Central) - Feb 17, 2022
Active, not recruiting --> Completed Our findings confirm that this data-driven systems pharmacogenomics strategy is a powerful approach for the discovery and validation of novel therapeutic candidates relevant to MB treatment, and along with data validating ixabepilone in PDX models of the two most aggressive subtypes of medulloblastoma, we present the network analysis framework as a resource for the field.
- |||||||||| paclitaxel / Generic mfg.
Journal: Microtentacle Formation in Ovarian Carcinoma. (Pubmed Central) - Feb 16, 2022
McTNs likely participate in key aspects of ovarian cancer metastasis. McTNs represent a new therapeutic target for this disease that could refine therapies, including intraperitoneal drug delivery.
- |||||||||| paclitaxel / Generic mfg.
Review, Journal: Microtubule-Interfering Drugs: Current and Future Roles in Epithelial Ovarian Cancer Treatment. (Pubmed Central) - Dec 27, 2021
In the past few years, epothilones (i.e., ixabepilone) have become of interest as they may retain activity in taxane-treated patients since they harbor several features that may overcome mechanisms of taxane resistance...Clinical data strongly support the use of microtubule-interfering drugs alone or in combination in the treatment of epithelial ovarian cancer. Ongoing clinical trials will shed further light into the potential of making these drugs part of current standard practice.
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