Inavolisib
A PI3Kα-targeted breast cancer drug — the chiral difluoromethyl oxazolidinone building block
Inavolisib — project profile
- Therapeutic area
- Oncology (breast cancer)
- Mechanism
- Selective PI3Kα inhibitor that also drives degradation of mutant PI3Kα
- Commercial status
- Marketed (FDA-approved first-line combination in Oct 2024)
- Originator
- Roche / Genentech
- Brand name
- Itovebi
Why this project, right now
Only publicly disclosed facts: regulatory approvals, clinical data, supply-chain moves
- ✓Roche won FDA approval for Itovebi in October 2024, in combination with palbociclib and fulvestrant, for endocrine-resistant, PIK3CA-mutated, HR-positive, HER2-negative locally advanced or metastatic breast cancer as detected by an FDA-approved test.
- ✓In the pivotal INAVO120 study the Itovebi-based regimen delivered median progression-free survival of 15.0 months versus 7.3 months with the control arm (HR=0.43; 57% reduction in the risk of progression or death). In January 2025 a statistically significant overall survival benefit was reported (HR=0.64).
- ✓PIK3CA mutations occur in roughly 40% of HR-positive metastatic breast cancers — the patient base makes this a durably growing product.
- ✓Three further Phase 3 studies (INAVO121, INAVO122, INAVO123) are ongoing, extending both indications and combinations.
Public regulatory and clinical milestones
| Date | Event |
|---|---|
| 2024-05 | FDA grants Priority Review and Breakthrough Therapy designation |
| 2024-10-10 | FDA approves the Itovebi + palbociclib + fulvestrant first-line regimen |
| 2025-01-28 | Significant overall survival benefit reported from INAVO120 (HR=0.64) |
Key intermediate list
1 key intermediates
| CAS No. | Chemical name | Fragment role | Action |
|---|---|---|---|
| 2059155-02-9 | (S)-4-(difluoromethyl)oxazolidin-2-one | Chiral difluoromethyl oxazolidinone fragment ((S)-configuration, CF2H) Process note：A small, high-value building block — optical purity and the difluoromethylation step define the process |
How we support this project
Supplied as the single (S)-enantiomer, with developed methods and data for ee, specific rotation and related substances
Tiered pricing by scale: gram samples → hundred-gram → kilogram, scaling up without a route change
Safety assessment for the difluoromethylation step and measured thermal-stability data from the partner plant
Common capabilitiesThe same delivery capability backs every campaign project
- ✓Route design and process development: hands-on scale-up experience with fluorinated, chiral, boronate and heterocyclic fragments at partner plants
- ✓Scale continuity: gram-scale validation → hundred-gram → kilogram → commercial, without a route change
- ✓Analytics: chiral ee, related substances, residual solvents, elemental impurities and genotoxic-impurity assessment to ICH conventions
- ✓Registration support: DMF feasibility assessment, starting-material justification, stability study design
- ✓Confidentiality: customer projects run under NDA; no cross-disclosure between plants and end customers
Supply scope and compliance note
Most of the target drugs above are originator products still under patent. The intermediates listed here are supplied for research use, and for markets where the patent has expired or a valid licence is in place. The buyer is responsible for confirming patent status and registration requirements in the target market and for the resulting compliance obligations. Third-party brand names and trademarks belong to their respective owners and are referenced here only as a technical cross-reference.
Intermediate lists (CAS and chemical names) are taken from the Division II 2026 Key Projects source sheet. Regulatory and clinical information comes from originator press releases and public FDA material. Fragment roles are neutral descriptions derived from the chemical structure and do not represent the originator patent route. Chinese drug names are common industry transliterations, not official registered names.
Data version 2026-09