Itovebi (inavolisib)
Research Synopsis
Itovebi (inavolisib)
An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms.
London, UK
2 hours ago
1 Received
- 1,3-Oxazole compounds are a type of five-membered ring chemicals containing nitrogen and oxygen, garnering interest in the fields of medicinal chemistry and pharmacology due to their varied structures and biological effects.
- Several 1,3-oxazole derivatives have been developed into medications, such as almoxatone and cabotegravir.
- This review summarizes 285 marine-derived 1,3-oxazole compounds, detailing their sources, structures, biological properties, biosynthesis, and chemical synthesis, while also offering insights into future discoveries in this area.
$100 - $150
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Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation.
London, UK
2 hours ago
1 Received
- The text discusses the p110α subunit of PI3Kα, a commonly activated kinase found in solid tumors.
- It highlights research by Song and colleagues showing that the PI3Kα inhibitors taselisib and inavolisib lead to the degradation of mutant p110α in breast cancer cells, specifically those that are HER2 positive.
- This degradation could help reduce drug resistance by limiting feedback from receptor tyrosine kinases (RTKs), potentially making PI3Kα inhibition more effective as a treatment option.
$100 - $150
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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy.
London, UK
2 hours ago
1 Received
- The p110a protein, a frequently mutated oncogene, is crucial for tumor growth, and new small-molecule inhibitors like GDC-0077 are showing promise in clinical trials for treating mutant breast cancer.
- Early studies highlight that while these inhibitors can effectively attack tumor cells, they may inadvertently activate compensatory signaling pathways that reduce their effectiveness.
- Recent findings reveal that GDC-0077 and taselisib uniquely degrade the mutant p110a protein, offering a more effective and targeted approach to inhibiting cancer pathways, especially in HER2-positive breast cancer patients.
$100 - $150
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Comparative molecular dynamics analyses on PIK3CA hotspot mutations with PI3Kα specific inhibitors and ATP.
London, UK
2 hours ago
1 Received
- * This study uses molecular dynamics simulations to analyze the interactions and binding affinities of PI3K inhibitors with specific PIK3CA hotspot mutations, revealing that alpelisib binds well, while inavolisib shows greater affinity for certain mutations.
- * The research highlights that specific mutations (like E542K) can drastically impair inhibitor interactions and affect the binding of natural ligands like ATP, which could influence the understanding of cancer mechanisms and aid in personalized medicine approaches.
$100 - $150
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
London, UK
2 hours ago
1 Received
- Small molecule inhibitors targeting the PI3K signaling pathway are being researched as cancer treatments, particularly for solid tumors linked to the PI3Kα isoform.
- The study focuses on developing benzoxazepin-oxazolidinone inhibitors that selectively degrade mutant p110α, the active part of PI3Kα, with impressive isoform specificity.
- The resulting clinical candidate, GDC-0077 (inavolisib), shows strong effectiveness in animal models and is currently in a Phase III clinical trial for treating patients with breast cancer harboring PI3Kα mutations.
$100 - $150
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Effective Combination Therapies for the Treatment of HER2 Cancer.
London, UK
2 hours ago
1 Received
- Breast cancer is the leading cause of cancer deaths in women globally.
- HER2-positive breast cancer makes up about 15% of cases and generally has a worse outlook.
- The patent discusses a combination treatment using inavolisib (GDC-0077) along with HER2-targeted therapies like trastuzumab or pertuzumab to improve outcomes for patients with HER2-overexpressing breast cancer.
$100 - $150
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Discovery of Unprecedented Human Stercobilin Conjugates.
London, UK
2 hours ago
1 Received
- - Two new metabolites (M18 and M19) derived from the drug inavolisib were found in the feces of human volunteers, indicating a significant alteration of the drug's structure after oral administration.
- - These metabolites were produced through reactions with stercobilin, a compound made by gut bacteria when breaking down heme, and involved both chemical and potentially enzymatic processes.
- - The study suggests a new mechanism for the formation of these metabolites and highlights their unique characteristics, potentially shedding light on similar drug interactions that may have been missed in earlier research.
$100 - $150
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Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models.
London, UK
2 hours ago
1 Received
- Estrogen receptor (ER) alpha is a key factor in ER+/HER2- breast cancer, and combining current therapies with new drugs is essential due to resistance issues like ESR1 mutations.
- Vepdegestrant (ARV-471) is a new drug that efficiently degrades both wild-type and mutant ER, showing significant tumor growth inhibition in various breast cancer models, outperforming the standard treatment fulvestrant.
- The study suggests that vepdegestrant could be a more effective treatment option for patients with ER+/HER2- breast cancer, especially when combined with other therapies like CDK4/6, mTOR, or PI3K inhibitors.
$100 - $150
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Phase I/Ib Trial of Inavolisib Plus Palbociclib and Endocrine Therapy for -Mutated, Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced or Metastatic Breast Cancer.
London, UK
2 hours ago
1 Received
- The study aimed to assess the safety, tolerability, and effectiveness of inavolisib combined with palbociclib and endocrine therapy for patients with specific types of breast cancer.
- A total of 53 patients participated, experiencing some treatment-related side effects, with common issues being stomatitis, hyperglycemia, and diarrhea, but overall the treatment was manageable.
- Results showed promising preliminary antitumor activity, with objective response rates of about 52% and 40%, and median progression-free survival of 23.3 and 35.0 months for different treatment combinations.
$100 - $150
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Preclinical Assessment of the PI3Kα Selective Inhibitor Inavolisib and Prediction of Its Pharmacokinetics and Efficacious Dose in Human.
London, UK
2 hours ago
1 Received
- * Inavolisib (GDC-0077) is a selective PI3Kα inhibitor that efficiently degrades mutated p110α proteins and has been studied for its absorption, distribution, metabolism, and excretion (ADME) characteristics.
- * Preclinical studies showed that inavolisib is effective against mutant KPL-4 breast cancer models, and predictions suggest a 3 mg dose could yield a clinical response; it is currently in phase 3 trials.
$100 - $150
Hourly Rate