Drug intelligence / Profile preview

azacitidine + paclitaxel

Development stage
Phase 2
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Azacitidine + paclitaxel is an investigational combination therapy consisting of two chemotherapeutic agents, azacitidine and paclitaxel. Azacitidine is a pyrimidine nucleoside analogue with hypomethylating and cytotoxic activity, primarily used in the treatment of myelodysplastic syndromes and acute myeloid leukemia. It inhibits DNA methyltransferase, leading to DNA hypomethylation and reactivation of silenced genes, as well as direct cytotoxicity through incorporation into RNA and DNA[2][6]. Paclitaxel is a taxane-class mitotic inhibitor that stabilizes microtubules, preventing cell division; it is widely used for various solid tumors including ovarian, breast, lung cancers[7]. The rationale for combining these drugs includes the ability of azacitidine to upregulate SPARC (an albumin-binding protein) in tumors via demethylation. This may enhance tumor accumulation of albumin-bound forms of paclitaxel (nab-paclitaxel), potentially increasing efficacy against solid tumors[1]. Early-phase clinical trials have shown promising activity in pre-treated cancer patients with manageable toxicity profiles[1].

02

Targets

DNMT (DNA methyltransferase)TUBB (Tubulin (alpha and beta subunits))

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