ZORTRESS (everolimus)
Zortress is an immunosuppressant used to prevent organ rejection in adults who have received a kidney or liver transplant. For kidney transplant patients at low-to-moderate risk, it is used alongside basiliximab, corticosteroids, and lower doses of cyclosporine. In liver transplant cases, the medication is started at least 30 days after the procedure and is used with corticosteroids and reduced doses of tacrolimus. This medication helps ensure the body does not reject the new organ by managing the immune response.
How ZORTRESS Works
This medication works by binding to a specific protein in cells called FKBP-12, creating a complex that inhibits the mammalian target of rapamycin (mTOR). By blocking this regulatory kinase, the drug prevents the activation and growth of T and B lymphocytes that would otherwise attack the transplanted organ. This process stops the synthesis of proteins necessary for cell proliferation, effectively reducing the risk of graft rejection.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2010-04-20
- Routes
- ORAL
- Dosage Forms
- TABLET
ZORTRESS Approval History
What ZORTRESS Treats
1 indicationsZORTRESS is approved for 1 conditions since its original approval in 2010. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Organ Rejection
ZORTRESS Boxed Warning
MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION Malignancies and Serious Infections Only physicians experienced in immunosuppressive therapy and management of transplant patients should prescribe Zortress. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information re...
WARNING: MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION Malignancies and Serious Infections Only physicians experienced in immunosuppressive therapy and management of transplant patients should prescribe Zortress. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient [see Warnings and Precautions (5.1)]. Increased susceptibility to infection and the possible development of malignancies, such as lymphoma and skin cancer, may result from immunosuppression [see Warnings and Precautions (5.2, 5.3)]. Kidney Graft Thrombosis An increased risk of kidney arterial and venous thrombosis, resulting in graft loss, was reported, mostly within the first 30 days posttransplantation [see Warnings and Precautions (5.4)]. Nephrotoxicity Increased nephrotoxicity can occur with use of standard doses of cyclosporine in combination with Zortress. Therefore, reduced doses of cyclosporine should be used in combination with Zortress in order to reduce renal dysfunction. It is important to monitor the cyclosporine and everolimus whole blood trough concentrations [see Dosage and Administration (2.4, 2.5), Warnings and Precautions (5.6), Clinical Pharmacology (12.7, 12.8)]. Mortality in Heart Transplantation Increased mortality, often associated with serious infections, within the first three months posttransplantation was observed in a clinical trial of de novo heart transplant patients receiving immunosuppressive regimens with or without induction therapy. Use in heart transplantation is not recommended [see Warnings and Precautions (5.7)]. WARNING: MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION See full prescribing information for complete boxed
ZORTRESS Target & Pathway
ProTarget
ZORTRESS Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
Drugs Similar to ZORTRESS
3 of 16FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
368 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT05773274 | NCI-2023-00118 NCI-2023-00118, CCTG-NE1 | Ph 2 | recruiting | Comparing Retreatment of 177Lu-DOTATATE PRRT Versus the Usual Treatment in Patients With Metastatic Unresectable Gastroenteropancreatic Neuroendocrine Tumors, NET RETREAT Trial |
| NCT04665739 | NCI-2020-12905 NCI-2020-12905, A021901 | Ph 2 | recruiting | Testing Lutetium Lu 177 Dotatate in Patients With Somatostatin Receptor Positive Advanced Bronchial Neuroendocrine Tumors |
| NCT07405164 | 6482-043 U1111-1325-4582, 2025-524160-38-00 | Ph 3 | recruiting | Extension Study for Participants in Studies That Include Belzutifan (MK-6482-043/LITESPARK-043) |
| NCT05918302 LEVEL | GETNE-T2217 2022-502154-13-00 | Ph 3 | recruiting | Efficacy and Safety of Radiotherapy Compared to Everolimus in Somatostatin Receptor Positive Neuroendocrine Tumors of the Lung and Thymus. |
| NCT04802759 | CO42867 2020-004889-19, 2023-507495-48-00 | Ph 1, Ph 2 | recruiting | A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer |
| NCT03577431 LITTMUS-MGH | DAIT ITN073ST | Ph 1, Ph 2 | active not recruiting | Liver Transplantation With Tregs at MGH |
| NCT07062965 | C4551002 2025-520566-22-00 | Ph 3 | recruiting | A Study to Learn About the Study Medicine Called PF-07248144 in Combination With Fulvestrant in People With HR-positive, HER2-negative Advanced or Metastatic Breast Cancer Who Progressed After a Prior Line of Treatment. |
| NCT06280950 ELIMINATE | DAIT CTOT-43 | Ph 2 | recruiting | Expanding Liver Transplant Immunosuppression Minimization Via Everolimus |
| NCT05306340 | ML43171 2022-000199-20, 2023-506821-12-00 | Ph 3 | active not recruiting | A Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With the Physician's Choice of Endocrine Therapy Plus Everolimus in Participants With Estrogen Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (evERA Breast Cancer) |
| NCT06428396 | 6482-029 MK-6482-029, LITESPARK-029 | Ph 2 | recruiting | Study of Belzutifan (MK-6482) Plus Fulvestrant for ER+/HER2- Metastatic Breast Cancer (MK-6482-029/LITESPARK-029) |
| NCT07165886 | HB1901-010 | Ph 2, Ph 3 | recruiting | Sirolimus for Injection (Albumin Bound) Combined With Octreotide Long-acting Injection in Patients With Metastatic Gastroenteropancreatic Neuroendocrine Tumors |
| NCT05843253 | CONNECT TarGeT-A R01FD008167 | Ph 2 | recruiting | Study of Ribociclib and Everolimus in HGG and DIPG or Ribociclib and Temozolomide in DHG, H3G34-mutant |
| NCT06943755 STELLAR-311 | XL092-311 2025-521043-20-00, 1011801 | Ph 2, Ph 3 | recruiting | Zanzalintinib Versus Everolimus in Participants With Locally Advanced or Metastatic Neuroendocrine Tumors |
| NCT04485559 | 190819 NCI-2020-04097 | Ph 1 | suspended | Trametinib and Everolimus for Treatment of Pediatric and Young Adult Patients With Recurrent Gliomas (PNOC021) |
| NCT02985125 results posted | 2016-0232 | Ph 1, Ph 2 | completed | LEE011 Plus Everolimus in Patients With Metastatic Pancreatic Adenocarcinoma Refractory to Chemotherapy |
| NCT01167530 RAD001 | IGR 1269 | Ph 1 | completed | Study to Evaluate RAD001 in Combination With Radiotherapy in Non-small Cell Lung Cancer |
| NCT07191353 StrongBone | 2024-520372-10-00 | Ph 2 | recruiting | Resistance Training and Rapamycin to Enhance Bone Formation in Postmenopausal Women |
| NCT06832189 EVEREST | DAIT ITN101ST | Ph 1 | recruiting | EVR and EPO for Liver Transplant Tolerance |
| NCT03049189 COMPETE results posted | ITM-LET-01 | Ph 3 | active not recruiting | Efficacy and Safety of 177Lu-edotreotide PRRT in GEP-NET Patients |
| NCT06382948 ADELA | MedOPP545 2024-512926-27-00 | Ph 3 | recruiting | Elacestrant + Everolimus in Patients ER+/HER2-, ESR1mut, Advanced Breast Cancer Progressing to ET and CDK4/6i. |
| NCT05252585 | CRAD001M2402 | Ph 4 | active not recruiting | A Phase IV Study of Safety and Efficacy of Everolimus in Taiwanese Patients With Tuberous Sclerosis Complex Who Have Renal Angiomyolipoma (TSC-AML) |
| NCT02962414 | CRAD001M2X02B 2024-516746-19-00 | Ph 3 | active not recruiting | Roll-over Study to Collect and Assess Long-term Safety of Everolimus in Patients With TSC and Refractory Seizures Who Have Completed the EXIST-3 Study [CRAD001M2304] and Who Are Benefitting From Continued Treatment |
| NCT05477576 ACTION-1 | RYZ101-301 | Ph 3 | recruiting | Study of RYZ101 Compared With SOC in Pts w Inoperable SSTR+ Well-differentiated GEP-NET That Has Progressed Following 177Lu-SSA Therapy |
| NCT05573126 | EP0062-101 | Ph 1, Ph 2 | recruiting | Phase 1/2 Study to Evaluate EP0062 as Monotherapy and in Combination in Patients With Advanced or Metastatic AR+/HER-2-/ER+ Breast Cancer |
| NCT03950609 | 2018-0253 NCI-2019-02051, 2018-0253 | Ph 2 | active not recruiting | Lenvatinib and Everolimus in Treating Patients With Advanced, Unresectable Carcinoid Tumors |
| NCT07477548 | 4-2025-1169 | Ph 2 | not yet recruiting | A Study to Evaluate the Efficacy and Safety of Everolimus in Patients With Teratment-refractory Vascular Anomalies |
| NCT05012371 | 2021-0400 NCI-2021-07429, 2021-0400 | Ph 2 | active not recruiting | Lenvatinib With Everolimus Versus Cabozantinib for Second-Line or Third-Line Treatment of Metastatic Renal Cell Cancer |
| NCT07426484 | 25-743 | Ph 4 | not yet recruiting | Cosibelimab for CSCC in Patients With Kidney Transplant or Hematologic Malignancy |
| NCT02811861 CLEAR results posted | E7080-G000-307 KEYNOTE-581, 2016-000916-14 | Ph 3 | active not recruiting | Lenvatinib/Everolimus or Lenvatinib/Pembrolizumab Versus Sunitinib Alone as Treatment of Advanced Renal Cell Carcinoma |
| NCT06105632 | C4391022 2023-506487-13-00 | Ph 2 | active not recruiting | A Study to Learn About the Study Medicine Called PF-07220060 in Combination With Fulvestrant in People With HR-positive, HER2-negative Advanced or Metastatic Breast Cancer Who Progressed After a Prior Line of Treatment |
| NCT02397083 LEVER | 2014-0944 NCI-2015-00919, 2014-0944 | Ph 2 | active not recruiting | Levonorgestrel-Releasing Intrauterine System With or Without Everolimus in Treating Patients With Atypical Hyperplasia or Stage IA Grade 1 Endometrial Cancer |
| NCT02143726 results posted | A091302 U10CA180821, NCI-2014-00623 | Ph 2 | active not recruiting | Sorafenib Tosylate With or Without Everolimus in Treating Patients With Advanced, Radioactive Iodine Refractory Hurthle Cell Thyroid Cancer |
| NCT03008408 | 2015-0961 NCI-2018-01284, 2015-0961 | Ph 2 | active not recruiting | A Phase II, Two-Arm Study of Everolimus and Letrozole, +/- Ribociclib (Lee011) in Patients With Advanced or Recurrent Endometrial Carcinoma |
| NCT01674140 e3 results posted | S1207 S1207, U10CA032102 | Ph 3 | active not recruiting | S1207 Hormone Therapy With or Without Everolimus in Treating Patients With Breast Cancer |
| NCT05949658 | 2023-0275 1U01AG081482-01, SMPH/MEDICINE/GER-AD DEV | Ph 1 | recruiting | Rapalog Pharmacology (RAP PAC) Study |
| NCT02520063 results posted | F150701004 (UAB 1514) UAB1514 | Ph 1, Ph 2 | completed | Combination of Letrozole, Everolimus and TRC105 in Postmenopausal Women With Hormone-Receptor Positive and Her2 Negative Breast Cancer |
| NCT05476939 BIOMEDE 2 | 2014/2126 2014-001929-32, 2023-506027-29-00 | Ph 3 | recruiting | Biological Medicine for Diffuse Intrinsic Pontine Glioma (DIPG) Eradication 2.0 |
| NCT01217931 | 2010-0085 NCI-2011-00256 | Ph 2 | active not recruiting | Sequential Two-agent Assessment in Renal Cell Carcinoma Therapy: The START Trial |
| NCT02407509 RAF/MEK | CCR3808 2012-001040-22 | Ph 1 | completed | Phase I Trial of VS-6766 Alone and in Combination With Everolimus |
| NCT02081755 | 013-307 | Ph 4 | enrolling by invitation | Safety and Efficacy of Everolimus Treatment in Liver Transplantation for Liver Cancer |
| NCT02057133 | 15252 I3Y-MC-JPBH | Ph 1 | active not recruiting | A Study of LY2835219 (Abemaciclib) in Combination With Therapies for Breast Cancer That Has Spread |
| NCT05933395 GERTRUDE | STUDY02001800 NCI-2024-09317 | Ph 2 | recruiting | Genetically-informed Therapy for ER+ Breast Cancer Post-CDK4/6 Inhibitor |
| NCT01087554 | 2009-0729 NCI-2011-00562 | Ph 1 | active not recruiting | Sirolimus or Everolimus or Temsirolimus and Vorinostat in Advanced Cancer |
| NCT02813135 ESMART | 2016-000133-40 2016/2396, 2024-514791-40-00 | Ph 1, Ph 2 | recruiting | European Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors |
| NCT03065387 | 2016-0430 NCI-2018-01218, 2016-0430 | Ph 1 | active not recruiting | Neratinib and Everolimus, Palbociclib, or Trametinib in Treating Participants With Refractory and Advanced or Metastatic Solid Tumors With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation |
| NCT05563220 ELEVATE | STML-ELA-0222 | Ph 1, Ph 2 | recruiting | Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer |
| NCT07318324 | 2025-1174 NCI-2025-09476 | Ph 1 | not yet recruiting | Phase Ib Study of Avutometinib, Defactinib, and Everolimus in RAS Pathway Mutant Endometrial Cancer |
| NCT00799188 CERTICOEUR | 2007.489/32 | Ph 3 | completed | CERTICOEUR: A Secondary Prevention Study of Skin Cancers in Heart Transplant Patients. Everolimus Versus Calcineurin Inhibitors Multicenter Trial |
| NCT03284957 AMEERA-1 results posted | TED14856 U1111-1189-4896, 2024-512997-89 | Ph 1, Ph 2 | terminated | Phase 1/2 Study of Amcenestrant (SAR439859) Single Agent and in Combination With Other Anti-cancer Therapies in Postmenopausal Women With Estrogen Receptor Positive Advanced Breast Cancer |
| NCT03740334 | 18-328 | Ph 1 | active not recruiting | Ribociclib in Combination With Everolimus and Dexamethasone in Relapsed ALL |
Showing 50 of 368 trials
Active Pipeline
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Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
ZORTRESS FDA Label Details
Indications & Usage
FDA Label (PDF)ZORTRESS is indicated for the treatment of Organ Rejection.
WARNING: MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION Malignancies and Serious Infections Only physicians experienced in immunosuppressive therapy and management of transplant patients should prescribe Zortress. Patients receivi...
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment