PTX-9908 / Pertinax Therapeutics, TCM Biotech - LARVOL DELTA

Necrosis-inducing peptide targeting CXCR4 suppresses breast cancer growth and metastasis (ACS-Fall 2025) - "In mice with syngeneic 4T-1 tumors, CTCE-KLAK significantly suppressed tumor growth and lung metastasis, whereas neither CTCE-9908 nor KLAK alone exhibited any antitumor effects. Only the peptide conjugate showed therapeutic efficacy.Our findings suggest that CTCE-KLAK, a CXCR4-targeted necrosis-inducing peptide, provides a novel cell death mechanism distinct from traditional apoptosis, offering potential as a therapeutic strategy for refractory TNBC."

Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CASP7 • ER • HER-2 • PARP1

Potential anti-metastatic properties of CTCE-9908 and L-kynurenine due to upregulation of cell-cell adhesion activity in a melanoma murine model (EADO-WCM 2025) - "A statistically significant increase in FAK expression in serum samples treated with CTCE/L-kyn and L-kynurenine was observed when compared to negative controls. Conclusions This study is the first to our knowledge to report on the anti-metastatic properties of CTCE-9908 and L-kyn in a melanoma mouse model by upregulating cell-cell adhesion activity."

Metastases • Preclinical • Genetic Disorders • Melanoma • Oncology • Skin Cancer • Solid Tumor • CDH1 • PTK2

In vitro Investigation of L-Kynurenine and Quinolinic Acid on Melanoma and Endothelioma Cells, and In Vivo Evaluation of L-Kynurenine Combined with CTCE-9908 in C57BL/6 Mice (EADO-WCM 2025) - "Conclusions L-kyn and Quin effectively inhibit melanoma and endothelioma cell proliferation in vitro. In vivo, L-kyn combined with CTCE-9908 shows therapeutic potential by significantly reducing tumour volume, warranting further research into its role in cancer treatment."

Preclinical • Melanoma • Oncology • Solid Tumor • ANXA5 • CASP3

A Study of PTX-9908 Injection for Non-resectable HCC with TACE (clinicaltrials.gov) - P1/2 | N=50 | Recruiting | Sponsor: TCM Biotech International Corp. | Trial completion date: Dec 2024 ➔ Dec 2026 | Trial primary completion date: Aug 2024 ➔ Aug 2026

Trial completion date • Trial primary completion date • Hepatocellular Cancer • Hepatology • Oncology • Solid Tumor

Preclinical evaluation of CXCR4 peptides for targeted radionuclide therapy in glioblastoma. (PubMed, EJNMMI Radiopharm Chem) - "In conclusion, we compared different 177Lu-radiolabelled CXCR4-targeting peptides for their binding potential in GBM, and demonstrated their varied cytotoxic action against GBM cells in vitro, with POL3026 being the most promising, causing considerable DNA damage. Though the peptide's systemic biodistribution remains to be improved, our data demonstrate the potential of [177Lu]Lu-DOTA-POL3026 for CXCR4-TRT in the context of GBM."

Journal • Preclinical • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor • CXCR4

In vitro effects and mathematical modelling of CTCE-9908 (a chemokine receptor 4 antagonist) on melanoma cell survival. (PubMed, Clin Exp Pharmacol Physiol) - "CTCE-9908 significantly inhibited melanoma cell survival at a concentration 10 times lower than the IC50 in B16 F10 cells but not RAW 264.7 cells. However, CTCE-9908 did not affect CXCR4 phosphorylation, apoptosis, or cell cycle distribution in either cell line."

Journal • Preclinical • Melanoma • Oncology • Solid Tumor • CASP3 • CXCL12

Hepatic Stellate Cell-Targeting Micelle Nanomedicine for Early Diagnosis and Treatment of Liver Fibrosis. (PubMed, Adv Healthc Mater) - "The SCLMs were firstly modified with peptide CTCE9908 (CT-SCLMs) and could actively target CXCR4, which is overexpressed in activated hepatic stellate cells...Furthermore, we took a step towards treatment by co-encapsulating two anti-fibrosis drugs, silibinin and sorafenib, within the CT-SCLMs...Symptoms associated with liver fibrosis, such as deposition of collagen, expression of hydroxyproline, and raised serological indicators showed notable improvement. In summary, the CXCR4-targeted nano-system can serve as a promising theragnostic system of early warning and diagnosis for liver fibrosis, offering hope against progression of this serious liver condition."

Journal • Fibrosis • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Immunology • Liver Cancer • Liver Cirrhosis • Liver Failure • Oncology • Solid Tumor

CXCR4-Targeted Necrosis-Inducing Peptidomimetic for Treating Breast Cancer. (PubMed, ACS Omega) - "Here, we have developed a CXCR4-targeted antitumor peptidomimetic (named CTCE-KLAK), which is a fusion of the CXCR4 receptor antagonist CTCE-9908 and the D-form of proapoptotic peptide (KLAKLAK), for the treatment of breast cancer...In addition, cell death by CTCE-KLAK was not prevented by z-VAD-fmk, a pan-caspase inhibitor that inhibits cisplatin-induced cell death...Intravenous administration of CTCE-KLAK significantly inhibited tumor growth and lung metastasis. Together, these findings suggest that the necrosis-inducing peptidomimetic CTCE-KLAK is a promising CXCR4-targeted agent for treating triple-negative breast cancer."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CASP3 • CASP7 • CXCR4 • PARP1

A Study of PTX-9908 Injection for Non-resectable HCC With TACE (clinicaltrials.gov) - P1/2 | N=50 | Recruiting | Sponsor: TCM Biotech International Corp. | Trial completion date: Dec 2023 ➔ Dec 2024 | Trial primary completion date: Aug 2023 ➔ Aug 2024

Trial completion date • Trial primary completion date • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Oncology • Solid Tumor

Vascular endothelial growth factor-C in activating vascular endothelial growth factor receptor-3 and chemokine receptor-4 in melanoma adhesion. (PubMed, J Cell Mol Med) - "CTCE-9908, a CXCR-4 antagonist derived from human CXCL12, hinders receptor phosphorylation and the subsequent signalling pathways that would be activated...In addition, increased VEGF-C protein levels lead to enhanced CXCR-4 protein expression. Therefore, effective blocking of VEGR-3 and CXCR-4 may inhibit tumour cell metastasis by hampering intracellular proteins promoting adhesion."

Journal • Review • Melanoma • Oncology • Solid Tumor • CXCL12 • CXCR4 • FLT4 • TGFB1 • VEGFA • VEGFC

The involvement of a chemokine receptor antagonist CTCE-9908 and kynurenine metabolites in cancer development. (PubMed, Cell Biochem Funct) - "For this reason, chemokines receptors represent potential targets for the treatment of cancer growth and metastasis. In this review paper, the role of the CXCL12/CXCR4 signalling pathway in the development of cancer is highlighted together with the current available treatments involving the CTCE-9908 compound in combination with microtubule inhibitors like paclitaxel and docetaxel."

Journal • Review • Genetic Disorders • Melanoma • Neuroblastoma • Oncology • Pediatrics • Skin Cancer • Solid Tumor • CXCL12

A Study of PTX-9908 Injection for Non-resectable HCC With TACE (clinicaltrials.gov) - P1/2 | N=50 | Recruiting | Sponsor: TCM Biotech International Corp. | Trial completion date: Dec 2021 ➔ Dec 2023 | Trial primary completion date: Aug 2021 ➔ Aug 2023

Trial completion date • Trial primary completion date • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Oncology • Solid Tumor

A Study of PTX-9908 Injection for Non-resectable HCC With TACE (clinicaltrials.gov) - P1/2; N=50; Recruiting; Sponsor: TCM Biotech International Corp.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open

A Study of PTX-9908 Injection for Non-resectable HCC With TACE (clinicaltrials.gov) - P1/2; N=50; Not yet recruiting; Sponsor: TCM Biotech International Corp.

Clinical • New P1/2 trial