Drug intelligence / Profile preview

alpelisib + luminespib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Alpelisib + luminespib** is a combination of two targeted small molecule drugs: - **Alpelisib** is a phosphatidylinositol 3-kinase (PI3K) alpha isoform inhibitor that suppresses PI3K/AKT/mTOR signaling, a pathway commonly activated in many cancers due to mutations such as PIK3CA. - **Luminespib** (code name AUY922) is a potent inhibitor of heat shock protein 90 (HSP90), a molecular chaperone required for stability and function of multiple oncogenic client proteins, including kinases and transcription factors relevant in cancer progression. This combination is investigated for synergistic anti-tumor activity, leveraging PI3K pathway blockade and inhibition of HSP90-dependent protein folding, which together may overcome resistance to monotherapies and inhibit tumor proliferation more effectively than either agent alone. The combination has been studied in early-phase clinical trials for advanced solid tumors, particularly those harboring PI3K pathway alterations or displaying resistance to monotherapy. Key adverse events are consistent with known toxicities of PI3K inhibitors (such as hyperglycemia, rash, gastrointestinal disturbances) and HSP90 inhibitors (ocular toxicity, liver enzyme elevations, gastrointestinal symptoms)[2].

Brand names
PIQRAY (alpelisib)
Other names
alpelisib + AUY922BYL719 + AUY922alpelisib + luminespib
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)HSP90AA1 (Heat shock protein HSP90-alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)HSP90AB1 (Heat shock protein HSP 90-beta)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CA (Phosphoinositide 3-kinase alpha)

Beyond the preview

Go deeper on alpelisib + luminespib.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on alpelisib + luminespib.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call