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- || Review, Journal: Research Progress of Targeted Therapy for Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma --Review (Pubmed Central) - Apr 25, 2024
At present, BTK inhibitors, PI3K inhibitors, spleen tyrosine kinase (SYK) inhibitors and BCL-2 inhibitors are the most studied targeted therapeutic drugs for CLL/SLL. This article reviews the research progress of different types of targeted therapeutic drugs in the treatment of CLL/SLL.
- | dactolisib (RTB101) / Adicet Bio
Preclinical, Journal: Reversal Effect of NVP-BEZ235 on Doxorubicin-Resistance in Burkitt Lymphoma RAJI Cell Line (Pubmed Central) - Apr 25, 2024
The constitutive activation of PI3K/AKT/mTOR pathway of RAJI/DOX cell line was more serious than RAJI cell line. NVP-BEZ235 reversed doxorubicin resistance of RAJI/DOX cell line by inhibiting the PI3K/AKT/mTOR signal pathway.
- | Journal, IO biomarker: Effect of Shikonin on Autophagy and Apoptosis of Human Promyelocytic Leukemia Cells (Pubmed Central) - Apr 25, 2024
NVP-BEZ235 reversed doxorubicin resistance of RAJI/DOX cell line by inhibiting the PI3K/AKT/mTOR signal pathway. Shikonin may promote autophagy and apoptosis of NB4 cells by inhibiting PI3K/Akt/mTOR pathway.
- | Journal: Discovery of Potent and Selective PI3K? Inhibitors for the Treatment of Acute Myeloid Leukemia. (Pubmed Central) - Apr 25, 2024
Thus, compound (S)-36 represents a promising PI3K? inhibitor for the treatment of acute myeloid leukemia with high efficacy.
- Piqray (alpelisib) / Novartis, Tukysa (tucatinib) / Pfizer
Interim safety analysis of phase IB trial of HER2 inhibitor tucatinib combined with PI3K? inhibitor alpelisib in HER2+ PIK3CA-mutated metastatic breast cancer. () - Apr 24, 2024 - Abstract #ASCO2024ASCO_6497;
P1/2
inhibitor for the treatment of acute myeloid leukemia with high efficacy. Clinical Trial Registration Number: NCT05230810
- RLY-2608 / Relay Therap
First-in-human study of RLY-2608, a pan-mutant and isoform selective PI3K? inhibitor, as a single agent in patients (pts) with advanced solid tumors and in combination with fulvestrant in pts with advanced breast cancer. (Hall A; Poster Bd #: 102a) - Apr 24, 2024 - Abstract #ASCO2024ASCO_2557;
P1
Clinical Trial Registration Number: NCT05230810 Clinical Trial Registration Number: NCT05216432
- Piqray (alpelisib) / Novartis
Sequential use of PI3K/AKT/mTOR pathway inhibitors alpelisib and everolimus in patients with hormone receptor-positive (HR+) metastatic breast cancer. (Hall A; Poster Bd #: 35) - Apr 24, 2024 - Abstract #ASCO2024ASCO_2487;
- risovalisib (CYH33) / HaiHe Biopharma
A phase Ib study of PI3K? inhibitor risovalisib mesylate in combination with fulvestrant in patients with PIK3CA-mutated, HR+/HER2- advanced breast cancer. (Hall A; Poster Bd #: 25) - Apr 24, 2024 - Abstract #ASCO2024ASCO_2478;
P1
Clinical Trial Registration Number: NCT05216432 Clinical Trial Registration Number: NCT04856371
- | Journal: Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. (Pubmed Central) - Apr 24, 2024
The adipoincretin effect operates in fasted mice with increasing FFA and decreasing glycemia, indicating that it is not primarily a control system for blood glucose. This feedback control system defines the rates of adipose tissue lipolysis and chiefly controls basal insulin secretion during fasting.
- | chlorogenic acid / Jiuzhang Biotech
Journal, IO biomarker: Exploring the neuroprotection of the combination of astragaloside A, chlorogenic acid and scutellarin in treating chronic cerebral ischemia via network analysis and experimental validation. (Pubmed Central) - Apr 24, 2024
These findings suggest that ACS against neuronal damage in cerebral ischemia may be closely related to the activation of PI3K/AKT pathway. These results declared first time ACS may become an ideal candidate drug against CCI due to its neuroprotective effects, which are mediated by the activated PI3K/AKT pathway mitigates mitochondrial damage and prevents cell apoptosis.
- || Review, Journal: Molecular targeted therapies for cutaneous squamous cell carcinoma: recent developments and clinical implications. (Pubmed Central) - Apr 24, 2024
The management of adverse events and toxicities in molecular-targeted therapies is crucial and requires careful monitoring and control. The paper further discusses future directions for therapeutic advancement and research in this area, as well as the difficulties and constraints associated with conventional therapies.
- | sirolimus / Generic mfg.
Journal: Explore the mechanism of astragaloside IV-PESV on proliferation, migration, and autophagy of prostate cancer cells based on the PI3K/AKT signaling pathway (Pubmed Central) - Apr 23, 2024
The paper further discusses future directions for therapeutic advancement and research in this area, as well as the difficulties and constraints associated with conventional therapies. The mechanism by which Astragaloside IV-Scorpion Venom Peptide inhibits the proliferation and migration of prostate cancer cells, suppresses cell mitosis, promotes early apoptosis, and enhances autophagy may be related to the inhibition of the PI3K/AKT pathway.
- || Preclinical, Review, Journal: Strategies and techniques for preclinical therapeutic targeting of PI3Kin oncology: where do we stand in 2024? (Pubmed Central) - Apr 22, 2024
We discuss the current landscape of PI3K inhibitors in preclinical and clinical trials, address the mechanisms of resistance to PI3K inhibition along with their associated toxic effects, and highlight significant advancements in preclinical research of this field. Based on our study and comprehension of PI3K, we provide a recapitulation of the key lessons learned from the research process and propose potential measures for improvement that could prove valuable.
- | tamoxifen / Generic mfg.
Journal, Epigenetic controller: Underlying anti-cancer mechanisms of histone deacetylase (HDAC) inhibitors in tamoxifen-resistant breast cancer cells. (Pubmed Central) - Apr 22, 2024
This study aimed to explore the underlying mechanisms of histone deacetylase (HDAC) inhibitor trichostatin A (TSA) to overcome resistance to tamoxifen in breast cancer cells...Finally, expression of vascular endothelial growth factor (VEGF), E-cadherin, Vimentin, phosphorylated phosphatidylinositol kinase (p-PI3k), phosphorylated protein kinase B (p-AKT), and phosphorylated mammalian target protein of rapamycin (p-mTOR) was evaluated by western blotting...However, HDAC inhibitor combined with PI3K inhibitor exerts more profound effects on the cancer cells as compared to HDAC inhibitor monotherapy. HDAC inhibitors inhibited the survival of breast cancer drug-resistant cells, invasion, migration, and angiogenesis by inhibiting the PI3k/Akt/mTOR signaling pathway.
- | Journal: Columbianadin suppresses glioblastoma progression by inhibiting the PI3K-Akt signaling pathway. (Pubmed Central) - Apr 22, 2024
Finally, we found that CBN inhibited GBM growth in an orthotopic mouse model of GBM through inhibiting PI3K/Akt signaling pathway. Together, these results suggest that CBN has an anti-GBM effect by suppressing PI3K/Akt signaling pathway, and is a promising drug for treating GBM effectively.
- | Journal: Physalin A Induces Apoptosis and Autophagy in Hepatocellular Carcinoma via Inhibition of PI3K/Akt Signaling Pathway. (Pubmed Central) - Apr 22, 2024
PA treatment inhibited tumor growth in tumor-bearing mice. PA triggers HCC cell apoptosis and autophagy by inactivating PI3K/Akt signaling.
- || Orserdu (elacestrant) / Menarini
Review, Journal: Novel oral selective estrogen receptor degraders (SERDs) to target hormone receptor positive breast cancer: Elacestrant as the poster-child. (Pubmed Central) - Apr 20, 2024
Elacestrant's recent approval sheds light on the use of biomarkers such as ESR1 to gauge a tumor's endocrine sensitivity. Ongoing therapeutic and correlative biomarker studies will offer new insight and expanding treatment options for patients with advanced breast cancer.
- Joenja (leniolisib) / Pharming Group
Off-label Treatment with the Selective PI3K? Inhibitor Leniolisib in 2 Pediatric Patients with Activated Phosphoinositide 3-kinase Delta Syndrome 2 (APDS2) () - Apr 19, 2024 - Abstract #CIS2024CIS_129;
- | LY294002 / Eli Lilly
Journal: Ginsenoside Rd Attenuates Myocardial Ischemia/Reperfusion Injury by Inhibiting Inflammation and Apoptosis through PI3K/Akt Signaling Pathway. (Pubmed Central) - Apr 18, 2024
The therapeutic effect of GRd in vivo and in vitro against myocardial I/R injury was primarily dependent on PI3K/Akt pathway activation to inhibit inflammation and cardiomyocyte apoptosis. This study provides new evidence for the use of GRd as a cardiovascular drug.
- | Aliqopa (copanlisib) / Bayer
Journal, Benefit-risk assessment: Model-Based Benefit/Risk Analysis for the Copanlisib Intermittent Dosing Regimen. (Pubmed Central) - Apr 18, 2024
Exposure-safety analyses revealed a borderline significant linear relationship for grade??3 TEAEs and no significant exposure-safety relationships for other investigated safety end points. The model-based benefit/risk framework considered the established exposure-response models and defined clinical utility function which confirmed the appropriateness of the copanlisib dosing regimen across the range of its achieved exposures.
- || STX-478 / Scorpion Therap
Trial completion date, Trial primary completion date, Combination therapy, Monotherapy, Metastases: STX-478-101: First-in-Human Study of STX-478 as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - Apr 17, 2024
P1/2, N=400, Recruiting, Sponsor: Scorpion Therapeutics, Inc.
The model-based benefit/risk framework considered the established exposure-response models and defined clinical utility function which confirmed the appropriateness of the copanlisib dosing regimen across the range of its achieved exposures. Trial completion date: Apr 2028 --> Feb 2029 | Trial primary completion date: Apr 2026 --> Feb 2027
- | Preclinical, Journal: The ACE2/Ang-(1-7)/MasR axis alleviates brain injury after cardiopulmonary resuscitation in rabbits by activating PI3K/Akt signaling. (Pubmed Central) - Apr 16, 2024
Inhibiting PI3K/Akt signaling inhibited Ang-(1-7)-mediated protection against brain damage after CA/CPR. Collectively, the ACE2/Ang-(1-7)/MasR axis alleviates CA/CPR-induced brain injury through attenuating hippocampal neuronal apoptosis by activating PI3K/Akt signaling.
- | buparlisib (AN2025) / Novartis, Adlai Nortye
Journal: Metformin and buparlisib synergistically induce apoptosis of non-small lung cancer (NSCLC) cells via Akt/FoxO3a/Puma axis. (Pubmed Central) - Apr 16, 2024
Moreover, they inhibited the PI3K/Akt signalling pathway, leading to activation of the FoxO3a/Puma signalling in NSCLC cells. Our findings suggest that combined treatment of metformin and buparlisib might provide a promising strategy for treating NSCLC.
- Test () - Apr 15, 2024 - Abstract #ERAEDTA2024ERA_EDTA_2707;
- | bleomycin / Generic mfg.
Journal: Qingkailing granule alleviates pulmonary fibrosis by inhibiting PI3K/AKT and SRC/STAT3 signaling pathways. (Pubmed Central) - Apr 15, 2024
In vivo, QKL reduced collagen deposition and suppressed proinflammatory cytokines in a bleomycin-induced PF mouse model...Molecular docking simulations highlighted interactions between QKL's active compounds and key proteins, showing inhibitory effects on epithelial damage and fibrosis. Collectively, these findings underscore the therapeutic potential of QKL in alleviating pulmonary inflammation and fibrosis through the downregulation of PI3K/AKT and SRC/STAT3 signaling pathways, with a pivotal role attributed to its active compounds.
- | pramipexole IR / Generic mfg., sirolimus / Generic mfg.
Preclinical, Journal: ?-Asarone inhibitsAutophagy by activating the PI3K/Akt/mTOR Pathway in a Rat Model of Depression in Parkinson's Disease. (Pubmed Central) - Apr 15, 2024
Collectively, these findings underscore the therapeutic potential of QKL in alleviating pulmonary inflammation and fibrosis through the downregulation of PI3K/AKT and SRC/STAT3 signaling pathways, with a pivotal role attributed to its active compounds. We concluded that ?-asarone might improve the behavior of DPD model rats by activating the PI3K/Akt/mTOR pathway, inhibiting autophagy and protecting neuron.
- | LY294002 / Eli Lilly
Journal: Cuscuta chinensis Lam. Flavonoids (CCLF) alleviate the symptoms of sepsis-associated encephalopathy via PI3K/Nrf2 pathway. (Pubmed Central) - Apr 15, 2024
LY294002, an inhibitor of PI3K, obviously blocked CCLF's functions on anti-apoptosis, anti-inflammation, and anti-oxidation in vivo, demonstrating that CCLF achieves its bioactivities in a PI3K/AKT signaling dependent manner. Altogether, CCLF exhibits remarkable neuro-protective function and may be a promising candidate for further clinical trials for SAE treatment.
- | Joenja (leniolisib) / Pharming Group
Journal: APDS patients with immune-complex vasculitis and resolution with leniolisib. (Pubmed Central) - Apr 15, 2024
IgA vasculitis resolved upon treatment with the inhibitor leniolisib. Patients with immune dysregulation including IgA vasculitis should be screened for APDS.
- | Journal: Network pharmacology analysis, molecular docking integrated experimental verification reveal ?-sitosterol as the active anti-NSCLC ingredient of Polygonatum cyrtonema Hua by suppression of PI3K/Akt/HIF-1? signaling pathway. (Pubmed Central) - Apr 15, 2024
We discovered Huangjing and its main active ingredient, ?-sitosterol, can reduce HIF-1?, AKT1, JUN and RELA expression and decrease non-small cell lung cancer growth through the PI3K/Akt/HIF-1? signaling pathway.
- | LY294002 / Eli Lilly, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Journal, PARP Biomarker: Geniposide ameliorates atherosclerosis by restoring lipophagy via suppressing PARP1/PI3K/AKT signaling pathway. (Pubmed Central) - Apr 13, 2024
Geniposide alleviated AS by restoring PARP1/PI3K/AKT signaling pathway-suppressed lipophagy. This study is the first to present the lipophagy-inducing effect of Geniposide and the binding of ABCG1 and PLIN1 inhibited by PARP1.
- | irinotecan / Generic mfg.
Journal: Ginsenoside Rh4 alleviates gastrointestinal mucositis and enhances chemotherapy efficacy through modulating gut microbiota. (Pubmed Central) - Apr 13, 2024
In summary, our findings confirm that ginsenoside Rh4 can alleviate CPT-11-induced gastrointestinal mucositis and enhance the anti-tumor activity of CPT-11 by modulating gut microbiota and its related metabolites. Our study validates the potential of ginsenoside Rh4 as a modulator of the gut microbiota and an adjunctive agent for chemotherapy, offering new therapeutic strategies for addressing chemotherapy side effects and improving chemotherapy efficacy.
- | Journal: Mitochondria-associated endoplasmic reticulum membranes tethering protein VAPB-PTPIP51 protects against ischemic stroke through inhibiting the activation of autophagy. (Pubmed Central) - Apr 12, 2024
Our findings suggest that the downregulation of VAPB-PTPIP51 expression after IS mediates structural damage to MAMs. This may exacerbate CIRI by inhibiting the PI3K pathway and activating autophagy, thus providing new therapeutic targets for IS.
- | Journal: MicroRNA-130b Suppresses Malignant Behaviours and Inhibits the Activation of the PI3K/Akt Signaling Pathway by Targeting MET in Pancreatic Cancer. (Pubmed Central) - Apr 12, 2024
Our findings illustrated the specific molecular mechanism of miR-130b regulating PC progress. The miR-130b/MET axis may be an alternative target in the therapeutic intervention of PC and provide an opportunity to deepen our understanding of the pathogenesis of PC.
- | Journal: Patients with acquired pure red cell aplasia respond to PI3K? inhibitor rapidly. (Pubmed Central) - Apr 12, 2024
The miR-130b/MET axis may be an alternative target in the therapeutic intervention of PC and provide an opportunity to deepen our understanding of the pathogenesis of PC. No abstract available
- | OT-82 / OncoTartis
Journal: A molecular circuit linking the BCR to the NAD biosynthetic enzyme NAMPT is an actionable target in Richter's syndrome. (Pubmed Central) - Apr 12, 2024
Lastly, treatment of RS-PDX mice with the combination of PI3Ki and OT-82 results in significant inhibition of tumor growth, with evidence of in vivo activation of apoptosis. Collectively, these data highlight a novel application for NAMPT inhibitors in combination with BTKi or PI3Ki in aggressive lymphomas.
- | Journal: Quercetin attenuates Pseudomonas aeruginosa-induced acute lung inflammation by inhibiting PI3K/AKT/NF-?B signaling pathway. (Pubmed Central) - Apr 11, 2024
Similarly, the in vitro study showed that the phosphorylation of these regulatory proteins and production of the proinflammatory cytokines were impaired in the quercetin-pretreated macrophages upon P. aeruginosa infection. Altogether, this study suggested that quercetin reduced the P. aeruginosa-induced acute lung inflammation by suppressing PI3K/AKT/NF-?B signaling pathway.
- | cordycepin (OVI-123) / OncoVista
Preclinical, Journal: Neuroprotective effects of cordycepin on MPTP-induced Parkinson's disease mice via suppressing PI3K/AKT/mTOR and MAPK-mediated neuroinflammation. (Pubmed Central) - Apr 10, 2024
In summary, our investigation reveals that cordycepin exerts neuroprotective effects against PD by promoting autophagy and suppressing neuroinflammation and neuronal apoptosis by inhibiting the PI3K/AKT/mTOR and ERK/JNK signaling pathways. This finding highlights the favorable characteristics of cordycepin in neuroprotection and provides novel molecular insights into the neuroprotective role of natural products in PD.
- | Journal: CPD-002, a novel VEGFR2 inhibitor, relieves rheumatoid arthritis by reducing angiogenesis through the suppression of the VEGFR2/PI3K/AKT signaling pathway. (Pubmed Central) - Apr 10, 2024
Mechanistically, CPD-002 hindered the activation of VEGFR2/PI3K/AKT pathway in VEGF-induced HUVECs and AIA rat synovium, as evidenced by reduced p-VEGFR2, p-PI3K, and p-AKT protein levels alongside elevated PTEN protein levels. Totally, CPD-002 showed anti-rheumatoid effects via attenuating angiogenesis through the inhibition of the VEGFR2/PI3K/AKT pathway.
- | Inlyta (axitinib) / Pfizer
Preclinical, Journal: Knockdown of the VEGFB/VEGFR1 signaling suppresses pubertal mammary gland development of mice via the inhibition of PI3K/Akt pathway. (Pubmed Central) - Apr 10, 2024
In this study, we observed that blocking the VEGF receptors with Axitinib suppressed the pubertal mammary gland development...Finally, the knockdown of VEGFB and VEGFR1 suppressed the pubertal development of mice mammary gland with the inhibition of the PI3K/Akt pathway. In summary, the results showed that knockdown of the VEGFB/VEGFR1 signaling suppresses pubertal mammary gland development of mice via the inhibition of the PI3K/Akt pathway, which provides a new target for the regulation of pubertal mammary gland development.
- | cisplatin / Generic mfg.
Journal: Differential modulation of PI3K/Akt/mTOR activity by EGFR inhibitors: A rationale for co-targeting EGFR and PI3K in cisplatin-resistant HNSCC. (Pubmed Central) - Apr 10, 2024
In summary, the results showed that knockdown of the VEGFB/VEGFR1 signaling suppresses pubertal mammary gland development of mice via the inhibition of the PI3K/Akt pathway, which provides a new target for the regulation of pubertal mammary gland development. Our data provided a rationale for EGFR inhibitors in combination with PI3K inhibitors to treat cisplatin-resistant HNSCC.
- | Preclinical, Journal, IO biomarker: Functionalized siRNA-chitosan nanoformulations promote triple-negative breast cancer cell death via blocking the miRNA-21/AKT/ERK signaling axis: in-silico and in vitro studies. (Pubmed Central) - Apr 9, 2024
The GE11-siRNA-CSNPs design, which specifically targets TNBC cells, offers a novel approach for the treatment of breast cancer with improved effectiveness. This study suggests that GE11-siRNA-CSNPs could be a promising candidate for further assessment as an additional strategy in the treatment of TNBC.
- | Journal: Dose optimization for cancer treatments with considerations for late-onset toxicities. (Pubmed Central) - Apr 9, 2024
We illustrate a re-design of this trial to compare the approach to those that only consider early toxicity outcomes and disregard late-onset toxicities. We also provide proposals going forward for dose optimization in early development of novel anticancer agents with considerations for late-onset toxicities.
- | Journal: Design of PI3K-mTOR Dual Inhibitors for Ovarian Cancer: Are We on the Right Track? (Pubmed Central) - Apr 8, 2024
Therefore, this review paves the way for finding an effective scaffold rather than the clinical part. The scaffold thus selected can be further modified and synthesized in the future as dual PI3K/mTOR inhibitors specifically for OC.
- | 5-fluorouracil / Generic mfg.
Journal: Wortmannin Inhibits Cell Growth and Induces Apoptosis in Colorectal Cancer Cells by Suppressing the PI3K/AKT Pathway. (Pubmed Central) - Apr 8, 2024
This study underscores Wortmannin's potential in inhibiting CRC cell growth and migration through PI3K/Akt pathway modulation. It also highlights its candidacy for further investigation as a promising therapeutic option in colorectal cancer treatment.
- | mefenamic acid / Generic mfg.
Preclinical, Journal: Mefenamic acid exhibits antitumor activity against osteosarcoma by impeding cell growth and prompting apoptosis in human osteosarcoma cells and xenograft mice model. (Pubmed Central) - Apr 8, 2024
Immunohistochemistry staining corroborated the in vivo findings, highlighting mefenamic acid's ability to suppress tumor proliferation and inhibit the PI3K/AKT/mTOR pathway within the tumor microenvironment. Collectively, these results underscore the promising therapeutic implications of mefenamic acid in combating osteosarcoma, warranting further investigation for clinical translation and development.
- | LY294002 / Eli Lilly
Journal: PI3K/AKT/mTORC1 signalling pathway regulates MMP9 gene activation via transcription factor NF-?B in mammary epithelial cells of dairy cows. (Pubmed Central) - Apr 8, 2024
-80?bp downstream from the transcription start site. These observations indicated that the PI3K/AKT/mTORC1 signalling pathway is involved in MMP9 expression by regulating MMP9 promoter activity via NF-?B in the mammary epithelial cells of dairy cows.
- | Journal: EphB3 receptor suppressor invasion, migration and proliferation in glioma by inhibiting EGFR-PI3K/AKT signaling pathway. (Pubmed Central) - Apr 8, 2024
These findings indicate that EphB3 functions as a tumor suppressor in glioma, and its downregulation enhances the malignant potential of glioma cells by activating the EGFR-PI3K/AKT pathway. Thus, EphB3 is a promising diagnostic marker for glioma, and the EphB3-EGFR-PI3K / AKT axis deserves further investigation as a potential therapeutic target.
- | Journal: MATN2 overexpression suppresses tumor growth in ovarian cancer via PTEN/PI3K/AKT pathway. (Pubmed Central) - Apr 7, 2024
These results indicated that MATN2 may play a critical role in ovarian cancer development by inhibiting cells proliferation and migration. The mechanism was related to interacting with PTEN, thus inhibiting downstream effectors in the PI3K/AKT pathway, which may be a novel target for treating ovarian cancer.
- | lapatinib / Generic mfg.
Journal: Lapatinib antitumor effect is associated with PI3K and MAPK pathway: An analysis in human and canine prostate cancer cells. (Pubmed Central) - Apr 6, 2024
Prostate cancer cells insensitive to androgens may be resistant to lapatinib through PI3K gene dysregulation. The association of lapatinib with PI3K inhibitors may provide a more effective antitumor response and clinical benefits to PC patients.
- || Piqray (alpelisib) / Novartis
Review, Journal: The PI3K/AKT/mTOR signaling pathway in breast cancer: Review of clinical trials and latest advances. (Pubmed Central) - Apr 6, 2024
Despite favorable efficacies, our analysis shows that the majority of trials are utilizing PI3K pathway inhibitors in combination with hormone therapy and chemotherapy; implying monotherapy cannot yield huge clinical benefits, at least partly, due to the activation of compensatory mechanisms. To emphasize the beneficial effects of these inhibitors in combined-modal strategies, we also reviewed recent studies which investigated the conjugation of nanocarriers with PI3K inhibitors to reduce harmful toxicities, increase the local concentration, and improve their efficacies in the context of BC therapy.