Drug intelligence / Profile preview

XL147 + paclitaxel + carboplatin

Development stage
Phase 2
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral (XL147), Intravenous (paclitaxel), Intravenous (carboplatin)
01

Overview

XL147 + paclitaxel + carboplatin is an experimental drug combination consisting of XL147 (also known as SAR245408 or pilaralisib), paclitaxel, and carboplatin. - **XL147** is a selective, orally available small molecule inhibitor of class I phosphoinositide 3-kinase (PI3K), which targets the PI3K/AKT/mTOR pathway. Inhibition of this pathway reduces cancer cell proliferation, survival, and resistance to therapies, including paclitaxel and carboplatin[1][2][3][4][6]. XL147 antagonizes PI3K pathway signaling by competitively inhibiting ATP binding in class I PI3Ks, leading to downstream inhibition of AKT, ribosomal S6 kinase, and ribosomal S6 protein, induction of apoptosis, inhibition of cell proliferation, and reduction in tumor growth. - **Paclitaxel** is a microtubule-stabilizing chemotherapy agent, disrupting cell division and inducing apoptosis. - **Carboplatin** is a platinum-based chemotherapy agent, causing DNA crosslinking and apoptosis in rapidly dividing cells[7]. This combination targets both the PI3K pathway (XL147) and mitosis/DNA integrity (paclitaxel, carboplatin) in solid tumors, and has been studied in phase 1 clinical trials for advanced solid tumors[1][3][5].

Other names
pilaralisib + paclitaxel + carboplatin
02

Targets

DNADNA-PK (DNA-dependent protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TUBB (Tubulin (alpha and beta subunits))PIK3C3 (PI3K class III)mTOR (Mammalian target of rapamycin kinase)

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