Eligible patients had disease progression on/after CDK4/6i + NSAI therapy and measurable disease per RECIST v1.1.8
*Prophylactic use of a steroid-containing mouthwash regimen was protocol mandated; oral nonsedating antihistamine therapy was recommended.8
| REVTORPYK triplet (n=131) |
REVTORPYK doublet (n=130) |
Fulvestrant (n=131) |
|
|---|---|---|---|
| Characteristic | |||
| Age, years, median (range) | 57 (33–83) | 57 (32–81) | 54 (28–83) |
| Female sex, n (%) | 129 (98.5) | 130 (100) | 128 (97.7) |
| Postmenopausal, n (%) | 101 (77.1) | 93 (71.5) | 92 (70.2) |
| Race/ethnic group, n (%) | |||
| White | 85 (64.9) | 95 (73.1) | 95 (72.5) |
| Asian | 18 (13.7) | 19 (14.6) | 25 (19.1) |
| Black or African American | 5 (3.8) | 3 (2.3) | 1 (0.8) |
| Other/unknown | 23 (17.6) | 13 (10.0) | 10 (7.6) |
| Geographic region, n (%) | |||
| United States/Canada | 21 (16.0) | 21 (16.2) | 22 (16.8) |
| Asia-Pacific | 18 (13.7) | 18 (13.8) | 26 (19.8) |
| Latin America | 35 (26.7) | 36 (27.7) | 35 (26.7) |
| Europe | 57 (43.5) | 55 (42.3) | 48 (36.6) |
| ECOG PS score, n (%) | |||
| 0 | 70 (53.4) | 85 (65.4) | 77 (58.8) |
| 1 | 61 (46.6) | 45 (34.6) | 54 (41.2) |
| REVTORPYK triplet (n=131) |
REVTORPYK doublet (n=130) |
Fulvestrant (n=131) |
|
|---|---|---|---|
| Characteristic, n (%) | |||
| Liver or lung metastases9 | 102 (77.9) | 104 (80.0) | 109 (83.2) |
| Prior (neo)adjuvant therapy, n (%) | |||
| Chemotherapy | 33 (25.2) | 39 (30.0) | 38 (29.0) |
| ET | 46 (35.1) | 57 (43.8) | 64 (48.9) |
| Prior lines, ET for aBC or mBC, n (%) | |||
| 0 | 3 (2.3) | 2 (1.5) | 4 (3.1) |
| 1 | 113 (86.3) | 113 (86.9) | 115 (87.8) |
| 2 | 15 (11.5) | 15 (11.5) | 12 (9.2) |
| Time to progression on immediate prior therapy, n (%) | |||
| ≤6 months | 21 (16.0) | 19 (14.6) | 20 (15.3) |
| >6 months | 109 (83.2) | 111 (85.4) | 111 (84.7) |
| Prior adjuvant CDK4/6i, n (%)9 | |||
| 3 (2.3) | 6 (4.6) | 4 (3.1) | |
| Prior CDK4/6i for aBC or mBC | |||
| Palbociclib, n (%) | 56 (42.7) | 47 (36.2) | 52 (39.7) |
| Ribociclib, n (%) | 59 (45.0) | 62 (47.7) | 70 (53.4) |
| Abemaciclib, n (%) | 23 (17.6) | 26 (20.0) | 16 (12.2) |
| Prior CDK4/6i for aBC or mBC, months, median duration (IQR) | 21.7 (13.7–35.0) | 18.1 (10.8–30.0) | 20.0 (12.0–34.2) |
AKTi=protein kinase B inhibitor; ECOG PS=Eastern Cooperative Oncology Group Performance Status; HbA1c=hemoglobin A1c; IQR=interquartile range; IV=intravenous; mTORi=mechanistic target of rapamycin inhibitor; NSAI=nonsteroidal aromatase inhibitor; PI3Ki=phosphoinositide 3-kinase inhibitor; T1DM=type 1 diabetes mellitus; T2DM=type 2 diabetes mellitus; TTP=time to progression.
IMPORTANT SAFETY INFORMATION
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.
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.
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. Afinitor. Prescribing information. Novartis Pharmaceuticals Corporation; 2025. 3. Layman RM, Han HS, Rugo HS, et al. Gedatolisib in combination with palbociclib and endocrine therapy in women with hormone receptor-positive, HER2-negative advanced breast cancer: results from the dose expansion groups of an open-label, phase 1b study. Lancet Oncol. 2025;25(4):474-487. 4. Itovebi. Prescribing information. Genentech USA, Inc; 2025. 5. Piqray. Prescribing information. Novartis Pharmaceuticals Corporation; 2024. 6. André F, Ciruelos E, Rubovszky G, et al; SOLAR-1 Study Group. Alpelisib for PIK3CA-mutated, hormone receptor-positive advanced breast cancer. N Engl J Med. 2019;380(20):1929-1940. 7. Truqap. Prescribing information. AstraZeneca Pharmaceuticals LP; 2025. 8. 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. 9. Hurvitz SA, Layman RM, Curigliano G, et al. Gedatolisib plus fulvestrant, with & without palbociclib, vs fulvestrant in patients with HR+/HER2-/PIK3CA wild-type advanced breast cancer: first results from VIKTORIA-1. Presented at: ESMO Congress; October 17-21, 2025; Berlin, Germany.