“The emerging role of capivasertib in breast cancer”

Activation of PI3K/AKT/mTOR Pathway Causes Drug Resistance in Breast Cancer

(2021) Chao Dong et al.   Frontiers in Pharmacology

Selective AKT kinase inhibitor capivasertib in combination with fulvestrant in PTEN-mutant ER-positive metastatic breast cancer

(2021) Lillian M. Smyth et al.   npj Breast Cancer

Concentration‐QT modeling shows no evidence of clinically significant QT interval prolongation with capivasertib at expected therapeutic concentrations

(2021) Veronika Voronova et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Phase 1b dose expansion and translational analyses of olaparib in combination with capivasertib in recurrent endometrial, triple negative breast, and ovarian cancer

(2021) Shannon N Westin et al.   CLINICAL CANCER RESEARCH

Outcome and molecular landscape of patients with PIK3CA-mutated metastatic breast cancer

(2020) F. Mosele et al.   ANNALS OF ONCOLOGY

Fulvestrant plus capivasertib versus placebo after relapse or progression on an aromatase inhibitor in metastatic, oestrogen receptor-positive breast cancer (FAKTION): a multicentre, randomised, controlled, phase 2 trial

(2020) Robert H Jones et al.   LANCET ONCOLOGY

Capivasertib, an AKT Kinase Inhibitor, as Monotherapy or in Combination With Fulvestrant in Patients With AKT1E17K-Mutant, ER-Positive Metastatic Breast Cancer

(2020) Lillian M Smyth et al.   CLINICAL CANCER RESEARCH

Genetic Alterations in the PI3K/AKT Pathway and Baseline AKT Activity Define AKT Inhibitor Sensitivity in Breast Cancer Patient-derived Xenografts

(2020) Albert Gris-Oliver et al.   CLINICAL CANCER RESEARCH

Phase I trial of the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib and AKT inhibitor capivasertib in patients with BRCA1/2 and non-BRCA1/2 mutant cancers

(2020) Timothy A. Yap et al.   Cancer Discovery

Circulating tumour DNA analysis to direct therapy in advanced breast cancer (plasmaMATCH): a multicentre, multicohort, phase 2a, platform trial

(2020) Nicholas C Turner et al.   LANCET ONCOLOGY

Effect of Capivasertib in Patients With an AKT1 E17K-Mutated Tumor

(2020) Kevin Kalinsky et al.   JAMA Oncology

BEECH: A dose-finding run-in followed by a randomised phase 2 study assessing the efficacy of AKT inhibitor capivasertib (AZD5363) combined with paclitaxel in patients with oestrogen receptor-positive advanced or metastatic breast cancer, and in a PIK3CA mutant sub-population

(2019) N C Turner et al.   ANNALS OF ONCOLOGY

PTEN Loss Mediates Clinical Cross-Resistance to CDK4/6 and PI3Kα Inhibitors in Breast Cancer

(2019) Carlotta Costa et al.   Cancer Discovery

Proliferation and AKT Activity Biomarker Analyses after Capivasertib (AZD5363) Treatment of Patients with ER+ Invasive Breast Cancer (STAKT)

(2019) John F.R. Robertson et al.   CLINICAL CANCER RESEARCH

Capivasertib Plus Paclitaxel Versus Placebo Plus Paclitaxel As First-Line Therapy for Metastatic Triple-Negative Breast Cancer: The PAKT Trial

(2019) Peter Schmid et al.   JOURNAL OF CLINICAL ONCOLOGY

A Phase 1, open-label, multicentre study to compare the capsule and tablet formulations of AZD5363 and explore the effect of food on the pharmacokinetic exposure, safety and tolerability of AZD5363 in patients with advanced solid malignancies: OAK

(2018) Emma Dean et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

E-cadherin loss induces targetable autocrine activation of growth factor signalling in lobular breast cancer

(2018) Katy Teo et al.   Scientific Reports

Targeting the BRD4/FOXO3a/CDK6 axis sensitizes AKT inhibition in luminal breast cancer

(2018) Jingyi Liu et al.   Nature Communications

AKT Inhibition in Solid Tumors With AKT1 Mutations

(2017) David M. Hyman et al.   JOURNAL OF CLINICAL ONCOLOGY

Co-treatment of LY294002 or MK-2206 with AZD5363 Attenuates AZD5363-induced Increase in the Level of Phosphorylated AKT

(2016) AE-RAN CHOI et al.   ANTICANCER RESEARCH

Safety and tolerability of AZD5363 in Japanese patients with advanced solid tumors

(2016) Kenji Tamura et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Landscape of Phosphatidylinositol-3-Kinase Pathway Alterations Across 19 784 Diverse Solid Tumors

(2016) Sherri Z. Millis et al.   JAMA Oncology

Validation of a predictive modeling approach to demonstrate the relative efficacy of three different schedules of the AKT inhibitor AZD5363

(2015) James W. T. Yates et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Combination AZD5363 with Enzalutamide Significantly Delays Enzalutamide-resistant Prostate Cancer in Preclinical Models

(2015) Paul Toren et al.   EUROPEAN UROLOGY

Combining AZD8931, a novel EGFR/HER2/HER3 signalling inhibitor, with AZD5363 limits AKT inhibitor induced feedback and enhances antitumour efficacy in HER2-amplified breast cancer models

(2015) CLAIRE CRAFTER et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

AKT Antagonist AZD5363 Influences Estrogen Receptor Function in Endocrine-Resistant Breast Cancer and Synergizes with Fulvestrant (ICI182780) In Vivo

(2015) R. Ribas et al.   MOLECULAR CANCER THERAPEUTICS

AKT inhibition synergistically enhances growth-inhibitory effects of gefitinib and increases apoptosis in non-small cell lung cancer cell lines

(2014) M. Puglisi et al.   LUNG CANCER

Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors

(2013) Eeva M. Sommer et al.   BIOCHEMICAL JOURNAL

The AKT inhibitor AZD5363 is selectively active in PI3KCA mutant gastric cancer, and sensitizes a patient-derived gastric cancer xenograft model with PTEN loss to Taxotere

(2013) Jing Li et al.   Journal of Translational Medicine

Synergistic Targeting of PI3K/AKT Pathway and Androgen Receptor Axis Significantly Delays Castration-Resistant Prostate Cancer ProgressionIn Vivo

(2013) Christian Thomas et al.   MOLECULAR CANCER THERAPEUTICS

Trastuzumab anti-tumor efficacy in patient-derived esophageal squamous cell carcinoma xenograft (PDECX) mouse models

(2012) Xianhua Wu et al.   Journal of Translational Medicine

Preclinical Pharmacology of AZD5363, an Inhibitor of AKT: Pharmacodynamics, Antitumor Activity, and Correlation of Monotherapy Activity with Genetic Background

(2012) B. R. Davies et al.   MOLECULAR CANCER THERAPEUTICS

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

An Integrative Genomic and Proteomic Analysis of PIK3CA, PTEN, and AKT Mutations in Breast Cancer

(2008) K. Stemke-Hale et al.   CANCER RESEARCH