CA102N / Holy Stone Healthcare - LARVOL DELTA

Mass balance, metabolic disposition, and pharmacokinetics of a single IV dose of [14C]CA102N in HT-29 xenograft athymic nude mice. (PubMed, Front Pharmacol) - "These findings demonstrated that metabolic clearance is the primary elimination pathway for CA102N and that the drug exhibits tumor retention, supporting its development as an anticancer therapy. Our results provided a strong pharmacological basis for the advancement of CA102N into the clinic."

Journal • PK/PD data • Preclinical • Metabolic Disorders • Oncology

Therapeutic efficacy of CA102N in pancreatic cancer (AACR 2024) - "Based on this compelling data, CA102N shows promise as a potential treatment for pancreatic cancer. Combination therapies and regimens are currently being explored in in vivo models as a strategy for clinical development."

Clinical • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • KRAS

[Announcement] HeBiotech’s new drug CA102N for the treatment of colorectal cancer has passed the human clinical trial review (IND) of the U.S. Food and Drug Administration (FDA) and was approved to conduct the second phase of human clinical trials [Google translation] (stock.yahoo) - "CA102N, a new drug used by HeBioTech to treat colorectal cancer, has passed the Human Clinical Trial Review (IND) of the U.S. Food and Drug Administration (FDA) and was approved to conduct Phase II human clinical trials....The US FDA applied for the second phase of human clinical trials on September 11, 2023, and received it on October 12, 2023."

IND • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Phase 2 Study of CA102N Combined With TAS-102 Compared to Bevacizumab Combined With TAS-102 in Subjects With Relapsed and/or Refractory Metastatic Colorectal Cancer (clinicaltrials.gov) - P2 | N=100 | Not yet recruiting | Sponsor: Holy Stone Healthcare Co., Ltd

Metastases • New P2 trial • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Phase 1 study of the safety, pharmacokinetics, and preliminary efficacy of CA102N as monotherapy and in combination with trifluridine-tipiracil in patients with locally advanced or metastatic solid tumors. (PubMed, Invest New Drugs) - P1 | "CA102N is a covalently bound conjugate of modified nimesulide (Nim) and NaHA, the sodium salt of hyaluronic acid (HA). (ClinicalTrials.gov registration number: NCT03616574. Registration date: August 6, 2018)."

Combination therapy • Journal • Monotherapy • P1 data • PK/PD data • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

First-in-human Study of CA102N Monotherapy and CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=37 | Completed | Sponsor: Holy Stone Healthcare Co., Ltd | Enrolling by invitation ➔ Completed

Monotherapy • Trial completion • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Individual Patient Expanded Access to CA102N (clinicaltrials.gov) - P=N/A | N=N/A | Available | Sponsor: Holy Stone Healthcare Co., Ltd

Combination therapy • New trial • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

First-in-human Study of CA102N Monotherapy and CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=33 | Enrolling by invitation | Sponsor: Holy Stone Healthcare Co., Ltd | Trial primary completion date: Dec 2021 ➔ Mar 2022

Monotherapy • Trial primary completion date • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

First-in-human Study of CA102N Monotherapy and CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=33; Enrolling by invitation; Sponsor: Holy Stone Healthcare Co., Ltd; Trial primary completion date: Sep 2021 ➔ Dec 2021

Clinical • Monotherapy • Trial primary completion date • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

First-in-human Study of CA102N Monotherapy and CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=33; Enrolling by invitation; Sponsor: Holy Stone Healthcare Co., Ltd; Recruiting ➔ Enrolling by invitation

Clinical • Enrollment status • Monotherapy • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

[VIRTUAL] Anticancer activity of CA102N in breast cancer cells in vitro and in vivo (AACR 2021) - "Combinations therapies and schedules are currently being explored in mice. to maximize the basis for its advancement therapy into the clinic."

Preclinical • Breast Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CD44

[VIRTUAL] CA102N suppresses the growth of mouse colon cancer by inhibition of PI3K pathway and immune modulation (AACR-II 2020) - "The reduction of tumor growth by CA102N in this particular tumor model was comparable to the mice having received TAS102 (100 mg/kg) p.o. daily for two weeks. Additionally, the protein expression of pAkt and pS6 in CA102N (200 mg/kg) treated tumor tissues were significantly down-regulated by more than 50% compared to that of control group, while CA102N (50 mg/kg) treatment only slightly altered the abundance of these proteins, suggesting antitumor activity of CA102N in different doses can potentially be mediated by differential mechanisms. Together, these findings suggest that the lower dose of CA102N exerts antitumor activity in mouse colon tumor model by immune modulation whereas the antitumor activity of the higher dose of CA102N might be mediated through inhibition of PI3kinase pathway on tumor tissues."

Preclinical • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CD8 • FOXP3 • IL6

First-in-human Study of CA102N Monotherapy and of CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=33; Recruiting; Sponsor: Holy Stone Healthcare Co., Ltd; Not yet recruiting ➔ Recruiting; Trial completion date: Jun 2021 ➔ Feb 2022; Trial primary completion date: Feb 2021 ➔ Sep 2021

Clinical • Enrollment open • Monotherapy • Trial completion date • Trial primary completion date