Side Effects of alpelisib: A Synthesis of Findings from 27 Studies

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Original Abstract of the Article

Major Research Findings

Alpelisib is an FDA-approved drug for treating advanced breast cancer with a mutation in the PIK3CA gene. 8 Alpelisib works by inhibiting PI3K, a key enzyme involved in cell growth and division. 10 When combined with fulvestrant, it can improve progression-free survival in patients with metastatic, hormone receptor-positive, PIK3CA-mutant breast cancer. 5 Alpelisib is also showing promise in treating PIK3CA-related overgrowth spectrum (PROS), a rare condition characterized by abnormal growth in various tissues, including the skin, bone, and connective tissue. 11

Reasons for Side Effects

PI3K plays a crucial role in various cellular functions, including cell growth, differentiation, metabolism, and immunity. 20 Therefore, alpelisib, by inhibiting PI3K, can affect not only cancer cells but also normal cells, leading to side effects. 10

Common Side Effects

Hyperglycemia

Hyperglycemia is a common side effect of alpelisib. 8 、 10 、 5 、 11 This is because PI3K is involved in insulin signaling, which regulates blood sugar levels. 10 、 17 When alpelisib inhibits PI3K, insulin function is weakened, leading to elevated blood sugar levels.

Rash

Alpelisib can cause skin side effects such as rash. 8 、 10 、 6 、 11 Rashes may be due to immune system activation by alpelisib or direct effects on skin cells. 4 These rashes can range from mild to severe, and in some cases, may lead to serious skin reactions such as Stevens-Johnson syndrome. 4

Diarrhea

Diarrhea is another side effect reported with alpelisib. 8 、 10 、 11 This may be due to PI3K's influence on cells in the digestive system. 11

Other Side Effects

Alpelisib may cause side effects in addition to hyperglycemia, rash, and diarrhea. 10 、 11 、 2 These include nausea, vomiting, loss of appetite, fatigue, weight loss, hair loss, mouth sores, pneumonia, liver damage, and kidney damage. 10

Side Effect Management

Hyperglycemia

Hyperglycemia from alpelisib can be managed through dietary and exercise adjustments, and by taking medications to lower blood sugar. 10 、 5 It's crucial to have your blood sugar levels monitored before starting alpelisib. 10 While taking alpelisib, you should get your blood sugar checked regularly and follow your doctor's instructions for treatment.

Rash

Mild rashes from alpelisib can often be treated with topical medications like steroid creams. 4 If the rash is severe, spreads to the whole body, or is accompanied by fever or fatigue, it might be necessary to stop taking alpelisib. 4

Diarrhea

Diarrhea from alpelisib is usually mild and often resolves within a few days. 11 If diarrhea is severe or prolonged, consult your doctor.

Comparison Across Studies

Commonalities Across Studies

Many studies have reported hyperglycemia, rash, and diarrhea as side effects of alpelisib. 8 、 10 、 5 、 6 、 11 These side effects appear to be relatively common.

Differences Across Studies

The frequency and severity of alpelisib's side effects can vary across studies. 10 Some studies have documented severe skin reactions such as Stevens-Johnson syndrome. 4 Individual factors, such as a patient's health and any other medications they are taking, can also affect how they experience alpelisib side effects.

Considerations for Real-World Application

Alpelisib is designed to benefit specific cancer patients with mutations in the PIK3CA gene. 8 Before considering alpelisib, consult your doctor to determine if it's the right treatment option for your condition and health. Regular checkups with your doctor are crucial while taking alpelisib. If you experience side effects like hyperglycemia, report them to your doctor promptly.

Current Research Limitations

Long-term side effects of alpelisib are not fully understood due to limited data. 10 Further research is needed to investigate how alpelisib interacts with other medications. 11

Future Research Directions

Research is needed to assess alpelisib's long-term safety and efficacy. 10 Developing new treatments to mitigate alpelisib side effects is also important. 4 Research should focus on optimizing alpelisib dosage and administration to minimize the risk of side effects. 2

Conclusion

Alpelisib has the potential to be an effective treatment option for specific cancer patients with PIK3CA gene mutations. 8 、 10 However, it's important to be aware of potential side effects such as hyperglycemia, rash, and diarrhea. 8 、 10 、 6 、 11 Before considering alpelisib, discuss your medical history and treatment options with your doctor to ensure it's the right choice for your individual needs. Regular checkups with your doctor are crucial for monitoring your health while taking alpelisib.

Keywords
Benefit Keywords
Blood pressure reduction
1
Improved quality of life
Improved symptoms
3
Breast cancer treatment
4
Breast cancer treatment
5
Breast cancer treatment
6
Improved efficacy in breast cancer
Maintains quality of life
Prolongs survival
7
Breast cancer treatment
8
Hyperglycemia
9
PIK3CA-mutated breast cancer treatment
10
PROS treatment
Prevents new lesions
Slows lesion progression
11
Breast Cancer Treatment
12
Breast cancer treatment
13
Partial response
14
Breast cancer treatment
PI3K inhibitor efficacy
15
PIK3CA-mutant cancer treatment
16
Aging treatment
17
Growth normalization
Prenatal diagnosis
Tissue regression
18
Inhibit PI3Kα mutants
Treats breast cancer
19
Cancer treatment
20
Cancer treatment
Targeted delivery
21
PIK3CA-mutated breast cancer treatment
22
Breast cancer prevention
23
Reduced drug dosage
Synergistic anti-cancer effect
24
CNS inflammation protection
Treg cell function
25
Cancer treatment
26
Prevent HO
27
Risk Keywords
Safety concerns
1
Breast cancer metastasis
Hyperglycemia
Liver metastases
2
Gastrointestinal side effects
Hyperglycemia
3
Alopecia
Rash
Stevens-Johnson Syndrome
4
Hyperglycemia
5
Vitiligo
6
Resistance to treatment
7
Diarrhea
Hyperglycemia
Rash
8
Alopecia
Decreased appetite
Diabetic ketoacidosis
Diarrhea
Fatigue
Nausea
Rash
Stomatitis
Vomiting
Weight loss
10
Cutaneous reactions
Diarrhea
Embryo-fetal toxicity
Hyperglycemia
Hypersensitivity
Pneumonitis
11
Diarrhea
Fatigue
Hyperglycemia
Nausea
Rash
14
Side effects
15
Side effects
19
Off-target effects
20
Alopecia
Decreased appetite
Diabetic ketoacidosis
Diarrhea
Fatigue
Nausea
Rash
Stomatitis
Vomiting
Weight loss
22
Antiestrogen side effects
23
Immune dysregulation
Treg cell loss
25
Side effects
26
Side effects
27
Literature analysis of 27 papers
Positive Content
22
Neutral Content
3
Negative Content
2
Article Type
0
1
0
6
23
1.

Clinical efficacy, safety and tolerability of aliskiren monotherapy: a protocol for an umbrella review.

Author: ZhaoQiyuan, ShenJiantong, LuJingya, LiFan, JiangQi, WangYuanyuan

Blood pressure reduction
Safety concerns

This paper systematically summarizes the published studies on the clinical efficacy and side effects of aliskiren monotherapy. Aliskiren, a renin-angiotensin-aldosterone system inhibitor, has been recognized for its role in lowering blood pressure. However, its safety and tolerability remain controversial.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Meta-AnalysisA statistical technique that integrates the results of multiple studies to draw more general conclusions about a particular issue.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

2.

Adverse events of alpelisib: A postmarketing study of the World Health Organization pharmacovigilance database.

Author: ChenXiao, WeiLianhui, ChiLijie, GuoXiaojing, ChenChenxin, GuoZhijian, LiangJizhou, ZhengYi, HeJia, YeXiaofei

Breast cancer metastasis
Hyperglycemia
Liver metastases

A disproportionality analysis of the VigiBase database identified several adverse events (AEs) potentially associated with alpelisib, including hyperglycemia, breast cancer metastasis, and metastases to liver. The most common AEs reported were hyperglycemia, rash, and diarrhea. Further monitoring and research are needed to understand the safety profile of alpelisib.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Case report: Alpelisib-induced Stevens-Johnson syndrome.

Author: KurianChristine Jane, DesaiAkshay, RaffertyWilliam, Abou HusseinAhmed Kamel

Breast cancer treatment
Alopecia
Rash
Stevens-Johnson Syndrome

Stevens-Johnson syndrome (SJS), a serious skin reaction, was reported in a patient receiving alpelisib for breast cancer. This is the first documented case of SJS associated with alpelisib.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

6.

Acrofacial vitiligo secondary to PI3KCA inhibitor, alpelisib: case report.

Author: HinichMaayan Geller, HijabAdham

Breast cancer treatment
Vitiligo

Alpelisib, a drug used to treat breast cancer, has been linked to a new case of vitiligo, a skin condition that causes depigmentation. This is the first reported case suggesting a causal relationship between alpelisib and irreversible skin adverse effects.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

8.

First Experiences with Alpelisib in Clinical Routine: Case Reports from a German Breast Center.

Author: HesterAnna, HenzeFranziska, TraviChristiane, HarbeckNadia, WuerstleinRachel

Breast cancer treatment
Diarrhea
Hyperglycemia
Rash

Alpelisib, a PI3K inhibitor, is the only approved treatment for PIK3CA-mutated, HR+, HER2- advanced breast cancer. Common side effects include hyperglycemia, diarrhea, and rash, with grade 3 severity reported in some cases.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

9.

SGLT2 inhibitors as potentially helpful drugs in PI3K inhibitor-induced diabetes: a case report.

Author: SahakianNicolas, CattieuwLauranne, Ramillon-CuryClotilde, CorrollerAudrey Bégu-Le, Silvestre-AillaudPascale, BéliardSophie, ValéroRené

Hyperglycemia

Hyperglycemia is a common side effect of phosphatidylinositol 3-kinase (PI3K) inhibitors used to treat breast cancer. This report describes the use of a sodium-glucose cotransporter 2 (SGLT2) inhibitor to manage severe hyperglycemia associated with PI3K inhibitor therapy.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

10.

Alpelisib-Induced Diabetic Ketoacidosis.

Author: NguyenPaul, MusaAya, SamantrayJulie

PIK3CA-mutated breast cancer treatment
Alopecia
Decreased appetite
Diabetic ketoacidosis
Diarrhea
Fatigue
Nausea
Rash
Stomatitis
Vomiting
Weight loss

Alpelisib, a drug for treating PIK3CA-mutated breast cancer, can cause diabetic ketoacidosis, highlighting the importance of monitoring blood glucose levels during treatment.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

12.

Efficacy of PI3K inhibitors in advanced breast cancer.

Author: VerretB, CortesJ, BachelotT, AndreF, ArnedosM

Breast Cancer Treatment

This review summarizes the current research on PI3K inhibitors in breast cancer, particularly focusing on alpelisib, the first PI3K inhibitor approved for the treatment of endocrine-resistant PIK3CA-mutant hormone receptor-positive tumors. The article explores potential future combinations of PI3K inhibitors for breast cancer patients.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

13.

Patient-Reported Outcomes in Patients With <i>PIK3CA</i>-Mutated Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer From SOLAR-1.

Author: CiruelosEva Maria, RugoHope S, MayerIngrid A, LevyChristelle, ForgetFrédéric, Delgado MingoranceJuan Ignacio, SafraTamar, MasudaNorikazu, ParkYeon Hee, JuricDejan, ContePierfranco, CamponeMario, LoiblSibylle, IwataHiroji, ZhouXiaolei, ParkJinhee, RidolfiAntonia, LorenzoInes, AndréFabrice

Breast cancer treatment

This study assessed health-related quality of life in patients with <i>PIK3CA</i>-mutated, hormone receptor-positive, HER2-negative advanced breast cancer who received alpelisib, a PI3Kα-selective inhibitor and degrader, in addition to fulvestrant. Alpelisib significantly improved progression-free survival in this population.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

15.

Efficacy of PI3K inhibitors in advanced breast cancer.

Author: VerretB, CortesJ, BachelotT, AndreF, ArnedosM

Breast cancer treatment
PI3K inhibitor efficacy
Side effects

This study reviews the research on PI3K inhibitors for breast cancer. It focuses on the role of the PI3K/Akt signaling pathway in breast cancer and highlights the potential of alpelisib, a specific PI3K inhibitor, in combination with fulvestrant.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

16.

Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

Author: FritschChristine, HuangAlan, Chatenay-RivaudayChristian, SchnellChristian, ReddyAnupama, LiuManway, KauffmannAudrey, GuthyDaniel, ErdmannDirk, De PoverAlain, FuretPascal, GaoHui, FerrettiStephane, WangYouzhen, TrappeJoerg, BrachmannSaskia M, MairaSauveur-Michel, WilsonChristopher, BoehmMarkus, Garcia-EcheverriaCarlos, ChenePatrick, WiesmannMarion, CozensRobert, LeharJoseph, SchlegelRobert, CaravattiGiorgio, HofmannFrancesco, SellersWilliam R

PIK3CA-mutant cancer treatment

This study investigated the biological properties of NVP-BYL719, a selective inhibitor of PI3Kα, a protein frequently mutated in solid tumors. The drug showed robust efficacy in PIK3CA-mutant cancers with acceptable side effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

17.

Efficacy of Providing the PI3K p110α Inhibitor BYL719 (Alpelisib) to Middle-Aged Mice in Their Diet.

Author: HedgesChristopher P, BoixJordi, JaiswalJagdish K, ShettyBhoopika, ShepherdPeter R, MerryTroy L

Aging treatment

BYL719 (alpelisib) is a drug that inhibits PI3K, a protein involved in cell growth and metabolism. This study investigated the long-term effects of BYL719 administered in the diet of mice. It showed that BYL719 effectively suppressed insulin signaling and did not have major toxicities or side effects, suggesting that dietary administration is suitable for studying its effects on aging and metabolism.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

18.

Early diagnosis enabling precision medicine treatment in a young boy with PIK3R1-related overgrowth.

Author: Schönewolf-GreulichBitten, KarstensenHelena Gásdal, HjortshøjTina D, JørgensenFinn Stener, HarderKatja M, FrevertSusanne, HoveHanne, DinessBirgitte R

Growth normalization
Prenatal diagnosis
Tissue regression

Alpelisib is a drug that blocks a protein called PIK3CA, which can cause overgrowth in some children. This study describes a child with overgrowth who was treated with alpelisib. The child's growth normalized and the affected tissues regressed.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

19.

PI3K inhibitors: review and new strategies.

Author: ZhangMingzhen, JangHyunbum, NussinovRuth

Inhibit PI3Kα mutants
Treats breast cancer
Side effects

This review explores the ongoing search for effective and specific inhibitors for PI3Kα mutants, a key lipid kinase involved in cancer development and drug resistance. The article discusses the limitations of current ATP-competitive PI3K inhibitors and proposes new therapeutic strategies, including the combination of allosteric and orthosteric inhibitors and utilizing allosteric rescue mutations to guide drug discovery.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

20.

Isoform-Selective PI3K Inhibitors for Various Diseases.

Author: BheemanaboinaRammohan R Y

Cancer treatment
Off-target effects

Isoform-selective PI3K inhibitors have emerged as promising therapeutic agents for cancer and other diseases. These inhibitors are crucial for understanding the unique functions of each PI3K isoform and its potential therapeutic applications.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

22.

Alpelisib-Induced Diabetic Ketoacidosis.

Author: NguyenPaul, MusaAya, SamantrayJulie

PIK3CA-mutated breast cancer treatment
Alopecia
Decreased appetite
Diabetic ketoacidosis
Diarrhea
Fatigue
Nausea
Rash
Stomatitis
Vomiting
Weight loss

Alpelisib, a drug for treating PIK3CA-mutated breast cancer, can cause diabetic ketoacidosis, highlighting the importance of monitoring blood glucose levels during treatment.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

23.

Short-term PI3K Inhibition Prevents Breast Cancer in Preclinical Models.

Author: KuAmy T, YoungAdelaide I J, IbrahimAhmed Atef, BuWen, JiangWeiyu, LinMeng, WilliamsLaterrica C, McCueBryant Lee, MilesGeorge, NagiChandandeep, BehbodFariba, LiYi

Breast cancer prevention
Antiestrogen side effects

Antiestrogen medications are the only chemoprevention options for high-risk women, but they have long-term treatment requirements and side effects. This study evaluated the potential of the PI3K inhibitor alpelisib for short-term chemoprevention of breast cancer. Alpelisib treatment prevented cancer formation in a mouse model and suppressed the expansion of atypical hyperplasia cells. Prophylactic targeting of PI3K activity could be a new strategy for breast cancer chemoprevention.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, Non-P.H.S.Research funding provided by US government agencies other than the Public Health Service.

Language : English

25.

Loss of Phosphatidylinositol 3-Kinase Activity in Regulatory T Cells Leads to Neuronal Inflammation.

Author: StarkAnne-Katrien, DavenportElizabeth C M, PattonDaniel T, ScudamoreCheryl L, VanhaesebroeckBart, VeldhoenMarc, GardenOliver A, OkkenhaugKlaus

CNS inflammation protection
Treg cell function
Immune dysregulation
Treg cell loss

PI3Kδ is crucial for Treg cell function, a type of immune cell that helps prevent autoimmune diseases. Blocking PI3Kδ can treat some cancers, but it can also cause immune problems. This study found that blocking both PI3Kα and PI3Kδ together worsened autoimmune disease in mice, highlighting the importance of PI3K signaling in immune regulation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

26.

Phase I study of alpelisib (BYL-719) and trastuzumab emtansine (T-DM1) in HER2-positive metastatic breast cancer (MBC) after trastuzumab and taxane therapy.

Author: JainSarika, ShahAmi N, Santa-MariaCesar A, SiziopikouKalliopi, RademakerAlfred, HelenowskiIrene, CristofanilliMassimo, GradisharWilliam J

Cancer treatment
Side effects

The combination of alpelisib and T-DM1 is tolerable and demonstrates activity in trastuzumab-resistant HER2-positive MBC. Activity was also observed in T-DM1-resistant disease. These data suggest that PIK3CA inhibition targets an important resistance pathway to anti-HER2 therapy.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

27.

Inhibition of phosphatidylinositol 3-kinase α (PI3Kα) prevents heterotopic ossification.

Author: ValerJosé Antonio, Sánchez-de-DiegoCristina, GámezBeatriz, MishinaYuji, RosaJosé Luis, VenturaFrancesc

Prevent HO
Side effects

This study found that BYL719, a PI3Kα inhibitor, effectively prevented heterotopic ossification (HO) in mice. BYL719 reduced SMAD, AKT, and mTOR/S6K activities, impairing skeletogenic responsiveness to BMPs and the acquired response to activin A of the Acvr1R206H allele. This research supports PI3Kα inhibition as a therapeutic strategy for HO.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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