Peptide
Plitidepsin (Aplidin)
Plitidepsin is a cyclic depsipeptide originally from Mediterranean marine tunicate Aplidium albicans, now synthesized. FDA/EMA orphan drug status for multiple myeloma. Approved in Australia (2018) for relapsed/refractory MM. Phase III trials ongoing for breast and lung cancers. Targets eEF1A2 protein overexpressed in cancer. Phase I/II: Demonstrated antitumor activity with tolerable safety. Enhanced efficacy with dexamethasone combination. Safe cardiac profile (1.9% drug-related cardiac AEs in 578 patients). Also studied for COVID-19.
- Updated
- How we grade
- 34 studies cited
Research notice. This page is for education and research. Peptides may not be FDA-approved for human use and may only be legally available for research. Talk to a qualified clinician before considering any peptide.
- Best evidence
- Grade A
- Conditions studied
- 2
- Outcomes
- 13
- Graded outcomes
- 1273
Evidence by condition
- Strong
- Moderate
- Limited
- Very limited
Cancer
General
| Grade | Outcome | Effect | Size | Studies | People | Studies list |
|---|---|---|---|---|---|---|
| COVID-19 Antiviral Activity In vitro and animal models: Significant reductions in SARS-CoV-2 viral load and pulmonary inflammation. Mechanism via eEF1A2 inhibition blocking viral replication. Clinical trials for COVID-19 application. | Improves (the measure goes up) | Moderate effect | 5 studies | |||
Studies that measured covid-19 antiviral activity
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Key findings
- Cardiac Safety ProfileImproves (the measure goes up)
- Anti-Cancer ActivityImproves (the measure goes up)
- Multiple Myeloma (with Dexamethasone)Improves (the measure goes up)
Studies cited
34 studies from PubMed
- Marine-Derived Compounds: A New Horizon in Cancer, Renal, and Metabolic Disease Therapeutics.
- Targeting eEF1A reprograms translation and uncovers broad-spectrum antivirals against cap or m(6)A protein synthesis routes.
- Functional characteristics of plitidepsin as an antiviral treatment against monkeypox virus infection.
- Can plitidepsin be used as an antiviral against RSV?
- Plitidepsin as an Immunomodulator against Respiratory Viral Infections.
- Outcomes and clinical characteristics of the compassionate use of plitidepsin for immunocompromised adult patients with COVID-19.
- Unraveling the antiviral activity of plitidepsin against SARS-CoV-2 by subcellular and morphological analysis.
- Marine Cyclic Peptides: Antimicrobial Activity and Synthetic Strategies.
- Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A
- Plitidepsin: Mechanisms and Clinical Profile of a Promising Antiviral Agent against COVID-19.
- Plitidepsin to treat multiple myeloma
- Generation of endoplasmic reticulum stress and inhibition of autophagy by plitidepsin induces proteotoxic apoptosis in cancer cells.
- Plitidepsin: design, development, and potential place in therapy
- Evaluation of plitidepsin in patients with primary myelofibrosis and post polycythemia vera/essential thrombocythemia myelofibrosis
- Evaluation of plitidepsin in patients with primary myelofibrosis and post polycythemia vera/essential thrombocythemia myelofibrosis: results of preclinical studies and a phase II clinical trial.
- Nano-encapsulation of plitidepsin: in vivo pharmacokinetics, biodistribution, and efficacy in a renal xenograft tumor model.
- Plitidepsin has a safe cardiac profile: a comprehensive analysis
- CXCR4-independent rescue of the myeloproliferative defect of the Gata1low myelofibrosis mouse model by Aplidin.
- Phase II study of weekly plitidepsin as second-line therapy for small cell lung cancer.
- Population pharmacokinetics meta-analysis of plitidepsin (Aplidin) in cancer subjects.
- Phase II randomized study of Plitidepsin (Aplidin), alone or in association with L-carnitine, in patients with unresectable advanced renal cell carcinoma.
- Phase I Clinical and Pharmacokinetic Study of Plitidepsin as a 1-Hour Weekly Intravenous Infusion in Patients with Advanced Solid Tumors
- Phase II study of plitidepsin in pretreated patients with locally advanced or metastatic non-small cell lung cancer.
- Phase I clinical and pharmacokinetic study of plitidepsin as a 1-hour weekly intravenous infusion in patients with advanced solid tumors.
- Plitidepsin has a dual effect inhibiting cell cycle and inducing apoptosis via Rac1/c-Jun NH2-terminal kinase activation in human melanoma cells
- Proteomic analysis of the resistance to aplidin in human cancer cells.
- Aplidin synergizes with cytosine arabinoside: functional relevance of mitochondria in Aplidin-induced cytotoxicity.
- Gateways to clinical trials.
- Oxidation and inactivation of low molecular weight protein tyrosine phosphatase by the anticancer drug Aplidin.
- Aplidin induces JNK-dependent apoptosis in human breast cancer cells via alteration of glutathione homeostasis, Rac1 GTPase activation, and MKP-1 phosphatase downregulation.
- Induction of resistance to Aplidin in a human ovarian cancer cell line related to MDR expression.
- Plitidepsin has a cytostatic effect in human undifferentiated (anaplastic) thyroid carcinoma.
- Aplidin induces apoptosis in human cancer cells via glutathione depletion and sustained activation of the epidermal growth factor receptor, Src, JNK, and p38 MAPK.
- In vitro cytotoxicity of aplidin and crossresistance with other cytotoxic drugs in childhood leukemic and normal bone marrow and blood samples: a rational basis for clinical development.