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REVTORPYK™ gedatolisib 180 mg for injection Logo
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REVTORPYK is administered on days 1, 8, and 15 of each 28-day cycle1

IV administration of REVTORPYK avoids first-pass exposure in the liver and GI tract and limits Cmax exposure to 3X per cycle1-5

IV infusion1

Recommended dose:

180 mg IV1

30-minute infusion1

No premedication required1*

3X per 28-day cycle1

Infrequent Cmax exposure

and long half-life of 36 hours1

*Initiate steroid-containing, alcohol-free mouthwash for oral prophylaxis at the start of treatment.1

REVTORPYK is given in combination with fulvestrant ± palbociclib1†

A combination regimen that targets the key pathways driving tumor cell proliferation1,6-9

28-day treatment schedule showing REVTORPYK dosing on days 1, 8, and 15 with fulvestrant and optional palbociclib

†Treatment may not include palbociclib.

Download the Dosing and
Administration Guide

Fulvestrant: Recommended dose is 500 mg administered as an intramuscular injection on day 1 of every cycle and day 15 of cycle 1 only10

Palbociclib (if prescribed): Recommended dose is 125 mg taken orally once daily for the first 21 days of each cycle11

Refer to the full Prescribing Information for fulvestrant and palbociclib for dosing information

Dosing modifications

Two dose reductions are recommended to help facilitate patient management1
Recommended starting dose
180 mg (20 mL reconstituted REVTORPYK)
First dose reduction
150 mg (17 mL reconstituted REVTORPYK)
Second dose reduction
130 mg (14 mL reconstituted REVTORPYK)

Permanently discontinue REVTORPYK in patients who are unable to tolerate 130 mg intravenously once weekly on days 1, 8, and 15 of every 28-day cycle1

Temporary interruption, dose reduction, or treatment discontinuation may be required for AR management, including:

  • Stomatitis
  • Hematologic toxicities
  • Dermatologic ARs
  • Hyperglycemia
  • Other ARs

Please see the REVTORPYK Dosing and Administration Guide or full Prescribing Information for more details on dosing modifications.

How to administer REVTORPYK1

1

Flush IV line with 5% Dextrose Injection before REVTORPYK administration.

2

Administer by IV infusion over 30 minutes through a dedicated infusion line equipped with a sterile, nonpyrogenic, in-line or add-on polyether sulfone filter (0.2- or 0.22-micron pore size) and catheter.

DO NOT administer any chloride-containing solutions or other medications concomitantly via the same IV line

3

Upon completion of the infusion, flush the IV line with 5% Dextrose Injection.

4

Discard any unused portions left in the infusion set.

Dosing line
See the safety profile of REVTORPYK Access resources for your practice

Cmax=maximum drug concentration; GI=gastrointestinal.

IMPORTANT SAFETY INFORMATION

WARNINGS AND PRECAUTIONS

Stomatitis: REVTORPYK can cause severe stomatitis, including ulcers and oral mucositis. Stomatitis occurred in 72% of patients treated with REVTORPYK with fulvestrant and palbociclib, including Grade 3 events in 22% of patients. Stomatitis occurred in 58% of patients treated with REVTORPYK with fulvestrant, including Grade 3 events in 12% of patients. Initiate a steroid-containing, alcohol-free mouthwash prior to starting treatment with REVTORPYK and continue prophylactically during treatment. Monitor patients for signs and symptoms of stomatitis. Withhold, reduce dose, or permanently discontinue REVTORPYK based on severity.

Dermatologic Adverse Reactions: REVTORPYK can cause severe rash. Rash occurred in 30% of patients treated with REVTORPYK in combination with fulvestrant and palbociclib, including Grade 3 events in 6% of patients. Rash occurred in 40% of patients treated with REVTORPYK with fulvestrant, including 5% of patients with Grade 3 events. Monitor patients for rash and infectious sequelae. Instruct patients to limit sun exposure during REVTORPYK treatment. Withhold, reduce dose, or permanently discontinue REVTORPYK based on severity.

Hyperglycemia: REVTORPYK can cause severe hyperglycemia. Monitor fasting glucose prior to initiating treatment with REVTORPYK and periodically during treatment. Monitor HbA1c level if clinically indicated. Increased fasting glucose occurred in 46% of patients receiving REVTORPYK in combination with fulvestrant and palbociclib (Grade 3: 0.9%) and in 57% of patients receiving REVTORPYK in combination with fulvestrant (Grade 3: 1.8%). The safety of REVTORPYK has not been established in patients with Type 1 or uncontrolled Type 2 diabetes mellitus. Patients with well-controlled Type 2 diabetes may require intensified antihyperglycemic therapy and close monitoring of fasting glucose. Manage hyperglycemia with antihyperglycemic medications as clinically indicated. Evaluate fasting blood glucose and HbA1c levels prior to starting and at regular intervals during treatment. Withhold, reduce dose, or permanently discontinue REVTORPYK based on severity.

Embryo-Fetal Toxicity: Based on its mechanism of action, REVTORPYK can cause fetal harm when administered to a pregnant woman. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with REVTORPYK and for 2 weeks after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 2 weeks after the last dose.

Advise women not to breastfeed during treatment with REVTORPYK and for 2 weeks after the last dose. When REVTORPYK is used in combination, advise patients to use effective contraception during treatment and for the longest post-treatment duration recommended in the Prescribing Information of any of the individual products. Verify the pregnancy status of females of reproductive potential prior to initiating treatment.

ADVERSE REACTIONS

REVTORPYK in Combination with Fulvestrant and Palbociclib: The most common (≥20%) adverse reactions, including laboratory abnormalities when given in combination with fulvestrant and palbociclib were decreased white blood cells, decreased neutrophils, decreased hemoglobin, decreased lymphocytes, stomatitis, nausea, decreased platelets, increased fasting glucose, fatigue, vomiting, rash, constipation, diarrhea, increased alanine aminotransferase (ALT), increased aspartate aminotransferase (AST), musculoskeletal pain, decreased sodium, and increased eosinophils.

REVTORPYK in Combination with Fulvestrant: The most common (≥20%) adverse reactions, including laboratory abnormalities when given in combination with fulvestrant were stomatitis, glucose increased, eosinophils increased, hemoglobin decreased, nausea, rash, ALT increased, fatigue, musculoskeletal pain, lymphocytes decreased, vomiting, AST increased, pruritus, and diarrhea.

INDICATION AND USAGE

REVTORPYK is a kinase inhibitor indicated in combination with fulvestrant, with or without palbociclib, for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer without a PIK3CA mutation detected following progression on or after treatment with at least one line of endocrine therapy in the metastatic setting.

INDICATION AND USAGE

REVTORPYK is a kinase inhibitor indicated in combination with fulvestrant, with or without palbociclib, for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer without a PIK3CA mutation detected following progression on or after treatment with at least one line of endocrine therapy in the metastatic setting.

Please see the full Prescribing Information for REVTORPYK.

You may report side effects to the FDA at (800) FDA-1088 or www.fda.gov/medwatch. You may also report side effects to Celcuity at 877-4-CELCUITY (877-423-5284).

References: 1. Revtorpyk. Prescribing information. Celcuity Inc; 2026. 2. Herman TF, Santos C. First-pass effect. In: StatPearls [Internet]. Treasure Island, FL: StatPearls Publishing; 2026. Updated November 3, 2023. Accessed June 6, 2026. https://www.ncbi.nlm.nih.gov/books/NBK551679/ 3. Houk BE, Alvey CW, Visswanathan R, et al. Distribution, metabolism, and excretion of gedatolisib in healthy male volunteers after a single intravenous infusion. Clin Pharmacol Drug Dev. 2019;8(1):22-31. 4. Shapiro GI, Bell-McGuinn KM, Molina JR, et al. First-in-human study of PF-05212384 (PKI-587), a small-molecule, intravenous, dual inhibitor of PI3K and mTOR in patients with advanced cancer. Clin Cancer Res. 2015;21(8):1888-1895. 5. Hurvitz SA, Layman RM, Curigliano G, et al. VIKTORIA-1 trial of gedatolisib plus fulvestrant with or without palbociclib in hormone receptor-positive/HER2-/PIK3CA wild-type advanced breast cancer. J Clin Oncol. 2026;44(12):1108-1119. 6. Clusan L, Ferrière F, Flouriot G, Pakdel F. A basic review on estrogen receptor signaling pathways in breast cancer. Int J Mol Sci. 2023;24(7):6834. 7. Finn RS, Aleshin A, Slamon DJ. Targeting the cyclin-dependent kinases (CDK) 4/6 in estrogen receptor-positive breast cancers. Breast Cancer Res. 2016;18(1):17. 8. Liu L, Graff SL, Wang Y. New emerging therapies targeting PI3K/AKT/mTOR/PTEN pathway in hormonal receptor-positive and HER2-negative breast cancer—current state and molecular pathology perspective. Cancers (Basel). 2024;17(1):16. 9. Rossetti S, Broege A, Sen A, et al. Gedatolisib shows superior potency and efficacy versus single-node PI3K/AKT/mTOR inhibitors in breast cancer models. NPJ Breast Cancer. 2024;10(1):40. 10. Faslodex. Prescribing information. AstraZeneca Pharmaceuticals LP; 2020. 11. Ibrance. Prescribing information. Pfizer Inc; 2025.