Alpelisib 150mg, 200mg, 250mg+50mg Film-Coated Tablets — PI3Kα-Selective Inhibitor for HR-Positive HER2-Negative PIK3CA-Mutated Advanced or Metastatic Breast Cancer in Combination With Fulvestrant
Pivikto® (Alpelisib) — First-in-Class PI3Kα Inhibitor for PIK3CA-Mutated HR+ HER2- Breast Cancer
The First PI3K Inhibitor Approved Specifically for Breast Cancer — Precision Therapy for the Most Common PIK3CA-Mutated Solid Tumour
Pivikto® (Alpelisib) is a first-in-class, selective inhibitor of the alpha isoform of phosphatidylinositol-3-kinase (PI3Kα) — the most frequently mutated kinase in human cancer. Alpelisib selectively targets PI3Kα while largely sparing PI3Kβ, PI3Kγ, and PI3Kδ isoforms — inhibiting the constitutively active PI3Kα enzyme produced by PIK3CA gain-of-function mutations that are found in approximately 40% of hormone receptor-positive (HR+) HER2-negative breast cancers.
By blocking mutant PI3Kα — the hyperactivated kinase that drives treatment resistance to endocrine therapy in PIK3CA-mutated breast cancer — Alpelisib restores sensitivity to hormonal treatment and suppresses the PI3K/AKT/mTOR signalling pathway that allows HR+ breast cancer cells to survive and proliferate despite estrogen deprivation. Used in combination with Faslodex (Fulvestrant) — a selective estrogen receptor degrader — Alpelisib provides dual blockade of both the ER pathway (Fulvestrant) and the PI3K escape pathway (Alpelisib) that cancer cells use to evade endocrine therapy.
Pivikto is approved for postmenopausal women and men with HR-positive, HER2-negative, PIK3CA-mutated, advanced or metastatic breast cancer in combination with Fulvestrant — after progression on or after an endocrine-based regimen. PIK3CA mutation testing by a validated companion diagnostic test is mandatory before prescribing.
A.K. Pharma is a trusted medicine distributor in Delhi supplying genuine Pivikto (Alpelisib) in all three tablet strengths — 150mg, 200mg, and 250mg+50mg — to hospitals, oncology centres, breast cancer clinics, and pharmacies across India. Manufactured by Novartis India Ltd, Pivikto is an essential precision oncology medicine for PIK3CA-mutated HR+ HER2- metastatic breast cancer — used alongside Faslodex (Fulvestrant) which is also available from A.K. Pharma.
What is Pivikto (Alpelisib)?
Pivikto contains Alpelisib — a small molecule 2-aminothiazole compound that acts as a selective, potent inhibitor of the PI3Kα catalytic subunit (encoded by PIK3CA) — the specific PI3K isoform most relevant to breast cancer oncogenesis.
The PI3K/AKT/mTOR Pathway — Central Driver of Endocrine Resistance in HR+ Breast Cancer:
The phosphatidylinositol-3-kinase (PI3K) pathway is one of the most frequently activated signalling cascades in human cancer. In HR+ breast cancer, this pathway is particularly important because:
Normal PI3K Signalling:
PIK3CA Mutations in Breast Cancer: PIK3CA activating mutations — most commonly H1047R, E545K, and E542K — are found in approximately 40% of HR+/HER2- breast cancers. These mutations create a constitutively hyperactive PI3Kα kinase that generates PIP3 continuously regardless of upstream growth factor signals → continuous AKT → mTOR activation → cancer cell survival, proliferation, and resistance to endocrine therapy.
Why PIK3CA Mutations Drive Endocrine Resistance: In the absence of estrogen (due to aromatase inhibitor or Fulvestrant therapy), HR+ breast cancer cells should undergo apoptosis. However, PIK3CA-mutant cells activate the PI3K/AKT/mTOR pathway as an alternative survival and proliferation route — bypassing ER dependence and enabling continued growth despite estrogen deprivation. This PI3K-driven bypass is the dominant mechanism of acquired endocrine resistance in HR+/HER2- breast cancer.
Alpelisib’s Mechanism — Restoring Endocrine Sensitivity: By selectively blocking mutant PI3Kα — Alpelisib eliminates the PI3K bypass mechanism. Combined with Fulvestrant blocking ER — the dual blockade leaves PIK3CA-mutant breast cancer cells with no functional proliferation or survival signal:
PI3Kα Selectivity — Why Isoform Selectivity Matters: Alpelisib’s selectivity for PI3Kα over other PI3K isoforms (PI3Kβ, PI3Kγ, PI3Kδ) is clinically important:
Full prescribing information is available at the FDA label for Alpelisib.
Clinical Studies and Evidence
SOLAR-1 Trial (Alpelisib + Fulvestrant in PIK3CA-Mutated HR+ HER2- Metastatic Breast Cancer) Published in the New England Journal of Medicine (2019), the landmark SOLAR-1 trial was a Phase 3 randomised controlled trial of 572 patients with HR-positive, HER2-negative, advanced breast cancer who had progressed on or after aromatase inhibitor therapy — comparing Alpelisib + Fulvestrant vs Placebo + Fulvestrant, with pre-specified analysis in the PIK3CA-mutated cohort. Key results in the PIK3CA-mutated cohort:
The SOLAR-1 trial established Alpelisib as the first PI3K inhibitor to demonstrate significant PFS benefit in breast cancer — and validated PIK3CA mutation testing as an essential companion diagnostic in HR+/HER2- metastatic breast cancer management.
BYLieve Trial (Alpelisib + Fulvestrant in Multiple Prior Therapy Settings) Published in The Lancet Oncology (2021), the BYLieve trial evaluated Alpelisib + Fulvestrant in three cohorts of patients with PIK3CA-mutated HR+/HER2- advanced breast cancer including those who had received prior CDK4/6 inhibitor therapy. Key results:
PIK3CA Mutation Testing — SOLAR-1 Biomarker Analyses: The SOLAR-1 trial definitively established that Alpelisib benefit is restricted to PIK3CA-mutated tumours. In the PIK3CA wild-type cohort, Alpelisib + Fulvestrant did not improve PFS vs Fulvestrant alone. This biomarker dependency makes PIK3CA testing mandatory before prescribing — only the PIK3CA-mutated population derives clinical benefit.
Available Strengths
Pivikto is available in the following tablet strengths:
| Presentation | Dose | Primary Use |
|---|---|---|
| Pivikto 150mg Film-Coated Tablets | 150mg | Standard starting dose tablets — three 150mg = standard 300mg dose (alternative) |
| Pivikto 200mg Film-Coated Tablets | 200mg | Dose combination — one 200mg + one 150mg = 350mg (dose escalation or titration step) |
| Pivikto 250mg+50mg Film-Coated Tablets | 300mg total (250+50) | Standard 300mg daily dose — two tablets per day (one 250mg + one 50mg) |
Standard approved dose: 300mg orally once daily with food — taken as one 250mg tablet + one 50mg tablet together.
All three strengths available from A.K. Pharma — enabling the standard 300mg dose and dose reduction steps.
Indications — What Pivikto is Used For
HR-Positive HER2-Negative PIK3CA-Mutated Advanced or Metastatic Breast Cancer:
Mandatory PIK3CA Mutation Testing: PIK3CA mutation status must be confirmed by a validated diagnostic test before prescribing Pivikto. Testing options:
Key PIK3CA hotspot mutations covered by Alpelisib: H1047R, H1047L, E545K, E542K, Q546R, E726K, C420R, and others — all conferring PI3Kα activation.
For detailed indication information refer to MedlinePlus Alpelisib.
Key Benefits of Pivikto
First and Only PI3K Inhibitor Approved for Breast Cancer Alpelisib is the first PI3K inhibitor to achieve regulatory approval in breast cancer — after multiple failed trials of pan-PI3K inhibitors that were limited by toxicity. The isoform selectivity of Alpelisib — targeting PI3Kα while sparing other PI3K isoforms — was the key advance that enabled clinically meaningful efficacy with a manageable safety profile.
Significant PFS Improvement in a Large and Clinically Important Population PIK3CA mutations are found in approximately 40% of HR+/HER2- metastatic breast cancers — one of the most common actionable molecular alterations in oncology. The SOLAR-1 trial demonstrates a significant PFS improvement — median 11.0 vs 5.7 months — in this large, molecularly defined population that was previously without a targeted therapy option beyond CDK4/6 inhibitors and endocrine agents.
Dual Blockade With Fulvestrant — Addressing Both Oncogenic Drivers Combining Alpelisib (PI3Kα blockade) with Faslodex (Fulvestrant) (ER degradation) addresses both oncogenic drivers simultaneously in PIK3CA-mutated HR+ breast cancer — the ER pathway that drives growth in estrogen-sensitive cells and the PI3K bypass pathway that enables endocrine resistance. Both medicines are available from A.K. Pharma.
Activity After CDK4/6 Inhibitor Progression The BYLieve trial demonstrates meaningful PFS with Alpelisib + Fulvestrant in patients who have progressed on CDK4/6 inhibitors — the current standard first-line therapy. As virtually all HR+/HER2- metastatic breast cancer patients now receive CDK4/6 inhibitors upfront, Alpelisib’s demonstrated activity in the post-CDK4/6i setting makes it directly relevant to the current treatment landscape.
Oral Once-Daily Dosing — Outpatient Management Single daily oral administration with food — no infusions required — allows complete outpatient management maintaining patient independence and quality of life.
All Three Strengths Available — Complete Dose Management A.K. Pharma supplies all three Pivikto strengths — 150mg, 200mg, and 250mg+50mg — enabling the standard 300mg daily dose and all dose reduction steps without sourcing from multiple suppliers.
How Pivikto Works — Selective PI3Kα Inhibition
Step 1 — Oral Absorption: Alpelisib is absorbed after oral administration with food — bioavailability is significantly higher when taken with a meal. Peak plasma concentration approximately 2 hours post-dose. Taking without food substantially reduces absorption — making the food administration requirement clinically important.
Step 2 — Selective PI3Kα Binding: Alpelisib enters cells and binds the ATP-binding site of the PI3Kα catalytic subunit (p110α) — competitively inhibiting ATP binding and blocking PI3Kα kinase activity. Alpelisib’s 2-aminothiazole scaffold provides selectivity for PI3Kα over PI3Kβ, PI3Kγ, and PI3Kδ through differential interactions in the binding pocket — selectivity that reduces immune cell toxicity while targeting the oncogenic isoform.
Step 3 — PIP3 Generation Blockade: With PI3Kα inhibited, the conversion of PIP2 to PIP3 at the cell membrane is blocked — PIP3 levels fall rapidly in PIK3CA-mutated cancer cells.
Step 4 — AKT/mTOR Pathway Suppression: Without PIP3 — AKT cannot be recruited to the membrane and phosphorylated by PDK1 → AKT is inactive → mTORC1 is not activated → S6K and 4E-BP1 phosphorylation falls → protein synthesis for cancer cell growth is suppressed → cancer cell cycle progression is blocked.
Step 5 — Elimination of PI3K Bypass Resistance: In PIK3CA-mutated cells previously treated with aromatase inhibitors or Fulvestrant, the PI3K bypass mechanism is eliminated. Without PI3K survival signals, cancer cells cannot sustain themselves on PI3K signalling alone — when Fulvestrant simultaneously eliminates ER signalling, PIK3CA-mutant cancer cells lose both survival pathways simultaneously.
Step 6 — Hyperglycaemia Mechanism: PI3Kα also mediates insulin-stimulated glucose uptake in muscle and adipose tissue. Alpelisib’s PI3Kα inhibition → reduced insulin-stimulated glucose uptake → compensatory insulin secretion → reactive hyperglycaemia. This on-target metabolic effect is the most clinically significant side effect of Alpelisib and requires proactive monitoring and management.
For detailed mechanism overview refer to ESMO Breast Cancer Guidelines and NCCN Breast Cancer Guidelines.
Pivikto + Faslodex — The Combination Regimen
Pivikto must always be used in combination with Faslodex (Fulvestrant) — not as monotherapy:
| Medicine | Brand | Dose | Route | Available at A.K. Pharma |
|---|---|---|---|---|
| Alpelisib (PI3Kα inhibitor) | Pivikto | 300mg once daily with food | Oral | Request Quote |
| Fulvestrant (SERD) | Faslodex | 500mg IM on Days 1, 15, 29 then monthly | IM injection | Request Quote |
Both components of the combination are available from A.K. Pharma — simplifying procurement for oncology centres managing PIK3CA-mutated metastatic breast cancer.
Dosage and Administration
Standard Dose:
Dose Reduction Schedule:
Hyperglycaemia Management — Critical: The most common reason for dose modification is hyperglycaemia. Pre-emptive management is essential:
Rash Management:
Monitoring Schedule:
| Parameter | Frequency |
|---|---|
| Fasting blood glucose (FBG) | Baseline; weekly × 2; then monthly |
| HbA1c | Baseline; every 3 months |
| LFTs | Baseline; periodically |
| CBC | Baseline; periodically |
| Lipase / Amylase | Baseline; periodically |
| Dermatological assessment | At every visit — rash monitoring |
| Renal function | Baseline; periodically |
Full dosing guidelines available at Drugs.com Alpelisib Dosage.
Who Should Use Pivikto
Pivikto is prescribed for:
PIK3CA testing mandatory before prescribing:
Patients Requiring Special Consideration:
Pivikto is prescribed by medical oncologists and breast cancer specialists. A.K. Pharma supplies Pivikto to hospitals, oncology centres, breast cancer clinics, and pharmacies across Delhi and India.
Possible Side Effects
Common side effects in the SOLAR-1 trial include hyperglycaemia (63.7% — the most common and clinically significant), diarrhoea (57.7%), rash (51.9%), nausea (44.5%), decreased appetite (35.6%), vomiting (26.6%), weight decrease (26.3%), stomatitis (29.8%), fatigue (29.5%), and alopecia (19.8%).
Hyperglycaemia — Most Important Side Effect: Grade 3-4 hyperglycaemia in approximately 36.6% — the most common reason for dose modification. Occurs due to on-target PI3Kα inhibition in insulin-signalling tissues. Proactive monitoring and anti-diabetic therapy management is essential — see dosage section above. Most cases are manageable with appropriate anti-diabetic therapy and dose reduction.
Rash: Grade 3 rash in approximately 19.2% — ranging from maculopapular rash to severe reactions. Proactive management with antihistamines and topical corticosteroids. Rare cases of Stevens-Johnson Syndrome (SJS), Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), and toxic epidermal necrolysis (TEN) reported — permanently discontinue for these severe reactions.
Diarrhoea: Grade 3 in approximately 6.7% — manage with loperamide, dietary modification, and dose reduction if severe.
Stomatitis: Oral mucositis in approximately 29.8% — manage with good oral hygiene, saline rinses, and topical analgesics. Grade 3 in approximately 5.4%.
Pneumonitis: Rare but serious — monitor for new or worsening respiratory symptoms. Withhold for Grade 2; permanently discontinue for Grade 3-4.
Full side effect information available at FDA Alpelisib Safety Information.
Precautions
Storage and Handling
As a responsible medicine distributor in Delhi, A.K. Pharma stores all medicines including Pivikto under manufacturer-recommended conditions ensuring product integrity for every supply.
Manufacturer Information
Pivikto (Alpelisib) is manufactured by Novartis India Ltd, the Indian subsidiary of Novartis AG. Alpelisib received FDA approval in May 2019 as Piqray — the first PI3K inhibitor approved for breast cancer — based on SOLAR-1 trial results. The Indian brand name is Pivikto. Available in strengths of 150mg, 200mg, and 250mg+50mg tablets. A.K. Pharma supplies only genuine Pivikto sourced from authorized Novartis India distributors.
Related Breast Cancer Medicines Available at A.K. Pharma
Frequently Asked Questions
Q. What is Pivikto used for? Pivikto (Alpelisib) is used in combination with Faslodex (Fulvestrant) to treat HR-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer in postmenopausal women and men who have progressed on or after endocrine-based therapy. PIK3CA mutation testing is mandatory before prescribing. More information at MedlinePlus.
Q. What is the generic name of Pivikto? Alpelisib. It is a selective PI3Kα inhibitor manufactured by Novartis India Ltd — the first PI3K inhibitor approved for breast cancer. The originator brand globally is Piqray (Novartis).
Q. Is PIK3CA mutation testing required before prescribing Pivikto? Yes — PIK3CA mutation testing by a validated diagnostic is mandatory. The SOLAR-1 trial demonstrated no benefit in PIK3CA wild-type tumours. Only patients with confirmed PIK3CA mutations benefit from Alpelisib. Testing can be performed on tumour tissue (NGS) or plasma (liquid biopsy using ctDNA).
Q. Can Pivikto be used alone without Fulvestrant? No — Pivikto is not approved as monotherapy. It must always be used in combination with Faslodex (Fulvestrant). The SOLAR-1 trial evaluated the combination — Alpelisib monotherapy without ER blockade is not a standard or approved approach.
Q. Why does Pivikto cause high blood sugar? PI3Kα mediates insulin-stimulated glucose uptake in muscle and fat tissue. When Alpelisib inhibits PI3Kα, this insulin-signalling process is impaired → glucose is not taken up efficiently → blood glucose rises (hyperglycaemia). This is an on-target metabolic effect of PI3Kα inhibition. Proactive blood glucose monitoring from Day 1 and early initiation of anti-diabetic therapy — typically metformin — is essential for managing this side effect.
Q. Can Pivikto be used after CDK4/6 inhibitor treatment? Yes — the BYLieve trial demonstrated clinically meaningful PFS benefit with Alpelisib + Fulvestrant in patients who had previously received CDK4/6 inhibitor therapy. As virtually all HR+/HER2- metastatic breast cancer patients now receive CDK4/6 inhibitors first-line, Alpelisib is increasingly relevant in the post-CDK4/6i setting.
Q. Must Pivikto be taken with food? Yes — Pivikto must be taken with a meal. Food significantly increases Alpelisib bioavailability. Taking without food substantially reduces absorption. Take consistently with a meal at the same time every day.
Q. What are the three strengths of Pivikto and how are they used? Pivikto is available as 150mg, 200mg, and 250mg+50mg tablets. The standard approved dose is 300mg once daily — taken as one 250mg tablet + one 50mg tablet together. The 150mg and 200mg tablets are used for dose reductions (first reduction 250mg; second reduction 200mg). All three strengths are available from A.K. Pharma.
Q. Is Pivikto available in India? Yes — Pivikto (Alpelisib 150mg, 200mg, 250mg+50mg) is available in India through licensed pharmaceutical distributors. Contact A.K. Pharma — medicine distributor in Delhi — for availability and pricing.
Q. What is the price of Pivikto in India? Pivikto price in India varies by strength and pack size. Contact A.K. Pharma at 011 4172 6999 or WhatsApp +91 9810034827 for current pricing.
Q. How to order Pivikto from A.K. Pharma? Request a quote from this page, call 011 4172 6999, or WhatsApp +91 9810034827. Please also enquire about Faslodex (Fulvestrant) when ordering Pivikto to procure both combination components together.
Q. Does A.K. Pharma supply Pivikto in bulk? Yes — in bulk to oncology centres, hospitals, and pharmacies across Delhi and India. Contact us for bulk pricing.
Why Order Pivikto from A.K. Pharma?
Contact A.K. Pharma for Pivikto Supply 📍 E-2/257A, 2nd Floor, Shastri Nagar, New Delhi 110052 📞 011 4172 6999 📱 WhatsApp: +91 9810034827 🌐 akpharma.in