Antineoplastic Peptides
9 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- Azurin-p28Azurin‑p28 (p28) is a 28‑amino‑acid peptide fragment derived from the bacterial redox protein azurin. It is being investigated as an investigational anticancer peptide that preferentially penetrates solid‑tumor cells and, in preclinical models, inhibits tumor growth by stabilising p53 and disrupting endothelial signalling. Research to date is limited to in‑vitro cell work, animal xenograft studies, and pharmacokinetic/toxicology profiling.
- CanfosfamideCanfosfamide (Telcyta, TLK286) is an investigational glutathione‑analog prodrug that is administered intravenously. It is being evaluated primarily for platinum‑refractory or -resistant ovarian cancer, where it is combined with pegylated liposomal doxorubicin or used as a third‑line single agent. The drug is activated inside tumour cells by glutathione‑S‑transferase P1‑1, leading to DNA damage and cell death.
- CIGB 300CIGB‑300 is an investigational cyclic peptide that blocks the activity of protein kinase CK2 by binding to the phospho‑acceptor domain of its substrates. Developed chiefly for locally advanced cervical cancer, it is delivered directly into tumours (intralesional) and has been evaluated in early‑phase clinical studies for safety and preliminary anti‑tumour activity.
- Dolastatin 10Dolastatin 10 is a marine‑derived pentapeptide that potently inhibits tubulin polymerisation, leading to cell‑cycle arrest and apoptosis. Although the naked compound has not been approved because its toxicity could not be separated from efficacy, its highly cytotoxic core has been repurposed as the payload for several antibody‑drug conjugates (ADCs) that are approved for certain lymphomas. Early laboratory work also identified nanomolar antiplasmodial activity.
- PNC-27Synthetic peptide derived from p53 residues 12-26 designed to target HDM-2 overexpressed on cancer cell surfaces, inducing selective cancer cell death without harming normal cells
- TallimustineTallimustine is an investigational antineoplastic peptide that belongs to the distamycin‑derived minor‑groove binders. It is a benzoyl nitrogen‑mustard analogue designed to alkylate adenine residues in AT‑rich DNA sequences, thereby interfering with gene transcription. Early clinical trials evaluated it for solid tumours, but development was halted because of pronounced bone‑marrow toxicity and limited tumour responses.
- TaltobulinTaltobulin (HTI‑286) is an investigational antimitotic peptide derived from the marine natural product hemiasterlin. It belongs to the antineoplastic peptide class and acts as a tubulin‑binding agent that disrupts microtubule polymerisation, leading to cancer cell death. Developed for intravenous administration, it is being explored as a potent cytotoxic payload for antibody‑drug conjugates and as a stand‑alone anticancer agent.
- TasidotinTasidotin (ILX651) is an investigational synthetic peptide derived from dolastatin‑15, developed as an antimitotic anticancer agent. It is administered intravenously and has been evaluated in early‑phase clinical trials for various advanced solid tumours. The compound targets microtubules to halt cell division, showing modest tumour responses and disease stabilisation in a limited number of patients.
- TyroserleutideTyroserleutide (YSL) is a synthetic tripeptide (tyrosyl‑seryl‑leucine) investigated as an antineoplastic agent, primarily for hepatocellular carcinoma. It is being studied in injectable form and within various nanocarrier systems for oral or targeted delivery. Pre‑clinical work shows tumor‑growth inhibition and survival benefits, while an early Phase I trial reported tolerability and modest clinical responses.