OnCo
drugsProductApproved2019🇪🇺🇬🇧🇯🇵🇨🇳🇦🇺

Alpelisib

Alpelisib was the first PI3K drug for PIK3CA-mutant breast cancer (2019). It is effective, but high blood sugar and rash limited its use, and newer drugs are displacing it.

SOLAR-1: PFS 11.0 vs 5.7 months with fulvestrant in PIK3CA-mutant disease. Hyperglycaemia (grade 3-4 ~37%), rash, and diarrhoea are frequent; requires metformin prophylaxis strategies. Superseded in first-line endocrine-resistant disease by inavolisib and in the unselected AKT-pathway-altered population by capivasertib.

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Alpelisib
PubChem
Modality
Small-molecule PI3Kα inhibitor
Mechanism
ATP-competitive PI3Kα-selective inhibitor.
Brand / code
Piqray
Dosing & schedule
Route
Oral
Schedule
300 mg once daily with fulvestrant
Dose modifications
Reduce to 250 then 200 mg for hyperglycaemia/rash
Monitoring
Fasting glucose and HbA1c before and during; antihistamine prophylaxis for rash
Medicare
Part D (self-administered)

Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).

Commercial insurance
covered with prior authorisation

Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy. PIK3CA mutation by an approved test required.

Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.

Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.

NICE recommendedNICE TA816 · 2022SMC: accepted
Appraised for
With fulvestrant for PIK3CA-mutated HR-positive, HER2-negative advanced breast cancer after a CDK4/6 inhibitor
NHS England
Routinely funded for the appraised indication (or via managed access)

Sources: NICE TA816 · SMC advice: alpelisib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.

Regulatory

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Approvals

RegionYearIndication
US2019PIK3CA-mutant HR+/HER2- advanced breast cancer with fulvestrant after endocrine therapy

Safety

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Toxicity profile
Adverse eventAny gradeGrade 3+
Hyperglycaemia
64%
37%
Diarrhoea
58%
7%
Rash
36%
10%

Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.

Trials

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ClinicalTrials.gov · phase 2/3
refreshed 2026-09-09
66 studies15 recruiting57 Phase 210 Phase 3
Search “Alpelisib” on ClinicalTrials.gov →
Counts are from a name search and may include unrelated studies; up to 100 studies are summarised.

Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
Alpelisib
intervention: Alpelisib
Open on ClinicalTrials.gov →

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Landmark trials in OnCo

Latest papers

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Literature trend123 papers in the last 12 months+14% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this drug: (TITLE:"Alpelisib" OR ABSTRACT:"Alpelisib" OR TITLE:"Piqray" OR ABSTRACT:"Piqray") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Alpelisib, not a curated reading list.

Connected

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