Cilengitide
From PeptidePlaza, the free peptide reference · Entry #1040 · Anti-Aging · Sources fetched 2026-09-10 · Editorial standards
Cilengitide (also known as EMD 121974, Cilengitida, cyclo(RGDf-N(Me)V), cilengitidum) is a anti-aging research peptide. Cilengitide is a cyclic RGD peptide and an integrin alpha-V/beta-3 and alpha-V/beta-5 antagonist, studied for various cancers.
Cilengitide, also known as EMD 121974, is a cyclic RGD peptide that functions as an antagonist of integrin alpha-V/beta-3 and integrin alpha-V/beta-5. It has been investigated in clinical trials for several types of cancer, reaching Phase 3 for glioblastoma. Other indications explored in Phase 2 include gliosarcoma, melanoma, astrocytoma, oligodendroglioma, non-small-cell lung carcinoma, castration-resistant prostatic neoplasms, and other brain neoplasms. Research on cilengitide often focuses on its role in cancer and the broader implications of integrins in cancer biology.
1 Mechanism of action
Integrin alpha-V/beta-3 antagonist (antagonist); Integrin alpha-V/beta-5 antagonist (antagonist)
2 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
2.1 Indicated / studied for
- Glioblastoma
- Gliosarcoma
- Melanoma
- Astrocytoma
- Oligodendroglioma
- Carcinoma, Non-Small-Cell Lung
- Prostatic Neoplasms, Castration-Resistant
- Brain Neoplasms
3 Chemical and physical properties
| CAS number | 188968-51-6 |
|---|---|
| Molar mass | 588.7 g/mol |
| Purity (typical) | Not independently verified |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
4 Research studies (8)
- Integrins in cancer: biological implications and therapeutic opportunities
Nature reviews. Cancer (2010) · Review - Spatial-reprogramming derived GPNMB(+) macrophages interact with COL6A3(+) fibroblasts to enhance vascular fibrosis in glioblastoma
Genome medicine (2025) - Inhibition of TGFβ1 activation prevents radiation-induced lung fibrosis
Clinical and translational medicine (2024) - Salvianolic acid B attenuates liver fibrosis by targeting Ecm1 and inhibiting hepatocyte ferroptosis
Redox biology (2024) - Type V Collagen in Scar Tissue Regulates the Size of Scar after Heart Injury
Cell (2020) - Targeting ITGβ3 to Overcome Trastuzumab Resistance through Epithelial-Mesenchymal Transition Regulation in HER2-Positive Breast Cancer
International journal of molecular sciences (2024) - ITGA5-expressing tumor cells interact with Schwann cells to drive nerve growth factor-mediated immunosuppression of NK cells
Molecular therapy : the journal of the American Society of Gene Therapy (2025) - Vitronectin-driven amyloid deposition disrupts mitochondrial homeostasis via integrin-mediated pathway in a humanized mouse model of transthyretin cardiac amyloidosis
European heart journal (2026)
5 Safety and risk profile
5.1 Regulatory status
Cilengitide is currently classified as Phase 3 clinical trials. It has no approved human indication in the United States; availability elsewhere does not imply demonstrated safety or efficacy.
6 Frequently asked questions
- What is Cilengitide?
- Cilengitide is a synthetic cyclic RGD peptide. It acts as an antagonist, specifically targeting and blocking the activity of integrin alpha-V/beta-3 and integrin alpha-V/beta-5 receptors.
- What is Cilengitide used for?
- Cilengitide has been studied in clinical trials for various cancers. It reached Phase 3 for glioblastoma and Phase 2 for conditions such as gliosarcoma, melanoma, astrocytoma, oligodendroglioma, non-small-cell lung carcinoma, castration-resistant prostatic neoplasms, and other brain neoplasms.
- How does Cilengitide work?
- Cilengitide works by acting as an antagonist for integrin alpha-V/beta-3 and integrin alpha-V/beta-5. By blocking these integrins, it interferes with their normal functions, which are often involved in processes like cell adhesion, migration, and angiogenesis, particularly relevant in cancer progression.
- What is the regulatory status of Cilengitide?
- Cilengitide has reached Phase 3 in clinical trials for glioblastoma. It has also been investigated in Phase 2 trials for several other cancer types, indicating its advanced stage of clinical development.
7 References
- Cilengitide — compound summary PubChem. View source
- Cilengitide — molecule record ChEMBL. View source
- Cilengitide — published literature (384 records) PubMed. View source
Related compounds
Entries that share a target, a mechanism, or a research area with Cilengitide.
Also anti-aging
A naturally occurring tripeptide-copper complex found in human plasma, saliva, and urine. Plasma levels decline sharply with age. Extensively studied for collagen induction, skin remodeling, and gene expression regulation.
Shares integrin and beta-3 pharmacology
Eptifibatide is an integrin alpha-IIb/beta-3 inhibitor used to decrease the rate of death or myocardial infarction in patients with acute coronary syndrome and those undergoing percutaneous coronary intervention.
Also anti-aging
Vasopressin is an FDA-approved peptide hormone and V1a, V1b, and V2 receptor agonist used to increase blood pressure in adults with vasodilatory shock.
Also anti-aging
The body's master antioxidant and the most abundant intracellular thiol. An unusual gamma peptide bond makes it resistant to normal peptidases — and its depletion tracks almost every disease of ageing.
Also anti-aging
The first drug that builds bone rather than merely slowing its loss — and it works only because it is given as a daily pulse. Continuous exposure to the same peptide destroys bone instead.
Also anti-aging
Desmopressin is a synthetic analog of vasopressin that acts as a vasopressin receptor agonist. It is FDA-approved for central diabetes insipidus and primary nocturnal enuresis.