Drug intelligence / Profile preview

NTQ1062 + fulvestrant

Development stage
Phase 3
Lead developer
Nanjing Chia-Tai Tianqing Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

NTQ1062 + fulvestrant is a combination therapy under clinical investigation for the treatment of advanced or metastatic hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer. NTQ1062 is an orally bioavailable, ATP-competitive small molecule inhibitor of Akt serine/threonine kinase 1 (AKT1), a key kinase in the PI3K-Akt-mTOR pathway that regulates tumor cell proliferation, survival, metabolism, metastasis, and invasion. Preclinical studies have shown that NTQ1062 exhibits potent antitumor activity in vitro and in vivo models with activated PI3K-Akt-mTOR signaling[6][8]. Fulvestrant is an estrogen receptor antagonist administered by intramuscular injection; it binds to and degrades estrogen receptors on breast cancer cells to block estrogen-driven tumor growth[1][4]. The combination aims to target both the hormonal driver (estrogen signaling) and downstream oncogenic pathways (Akt), potentially overcoming resistance mechanisms in HR-positive/HER2-negative breast cancer patients who have failed standard treatments[5][7].

02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)ESR1 (ERα)ESR2 (ERβ)AKT (RAC-alpha serine/threonine-protein kinase)

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