Delving into the Latest Updates on CA-102N with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Akt x CD44 x ERK x MEK x PI3Ks x mTOR

Action

inhibitors

Mechanism

Akt inhibitors(Proto-oncogene proteins c-akt inhibitors), CD44 inhibitors(CD44 antigen inhibitors), ERK inhibitors(ERK subfamily inhibitors)

+ [3]

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [2]

Active Indication

Metastatic Colorectal CarcinomaBladder CancerPancreatic Ductal Adenocarcinoma+ [1]

Inactive Indication

Locally Advanced Malignant Solid NeoplasmNeoplasm Metastasis

Originator Organization

Holy Stone Healthcare Co., Ltd.

Active Organization

Holy Stone Healthcare Co., Ltd.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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HS-CA102N-103 is a Phase 2, randomized, open label study to evaluate efficacy, safety, and tolerability of CA102N combined with trifluridine/tipiracil (TAS-102) compared to bevacizumab combined with TAS-102 in subjects with metastatic colorectal cancer (mCRC) who failed the standard treatment (for eg, cancer that has relapsed after or is refractory to fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy).

Start Date01 Jan 2024

Sponsor / Collaborator

Holy Stone Healthcare Co., Ltd.

NCT03616574

/ CompletedPhase 1

Phase 1,Two-part (Dose Escalation, Dose Expansion), Multicenter,Non-randomized,Open-label, Multiple Dose, First-in-human Study of CA102N Monotherapy and of CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors

Study HS-CA102N-101 is a phase 1, two part (dose escalation, dose expansion), multicenter, non-randomized, open-label, multiple dose, first-in-human study of CA102N monotherapy and of CA102N combined with trifluridine/tipiracil (LONSURF) in subjects with advanced solid tumors.
CA102N will be evaluated in subjects with locally advanced or metastatic solid tumours for which no effective therapy is available in Part 1 (dose escalation) and in subjects with relapsed or refractory locally advanced or metastatic colorectal cancer (mCRC) after prior oxaliplatin and irinotecan-based chemotherapy in Part 2 (dose expansion).

Start Date09 Apr 2019

Sponsor / Collaborator

Holy Stone Healthcare Co., Ltd.

100 Clinical Results associated with CA-102N

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100 Translational Medicine associated with CA-102N

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100 Patents (Medical) associated with CA-102N

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1

Literatures (Medical) associated with CA-102N

01 Feb 2023·Investigational New Drugs

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

Article

Author: Pant, Shubham ; Kopetz, Scott ; Jimeno, Antonio ; Chen, Yuchih C ; Tchaparian, Eskouhie ; Dragovich, Tomislav ; Lieu, Christopher ; Menter, David ; Kundranda, Madappa

CA102N is a covalently bound conjugate of modified nimesulide (Nim) and NaHA, the sodium salt of hyaluronic acid (HA). HA is a natural ligand of cluster of differentiation 44 (CD44), which is over-expressed in colorectal cancer (CRC). CA102N is designed to deliver nimesulide directly to the tumor via the interaction of HA and CD44. A Phase 1, 2-part (dose escalation, dose expansion), non-randomized, open-label, first-in-human study of CA102N, as monotherapy and in combination with trifluridine-tipiracil, was conducted in patients with locally advanced or metastatic solid tumors. The CA102N doses evaluated were 0.36 mg/kg, 0.54 mg/kg, and 0.72 mg/kg Nim equivalent. The primary endpoints were dose-limiting toxicities (DLTs) in Cycle 1 as well as serious adverse events (SAEs) and treatment-emergent adverse events (TEAEs) throughout the study; secondary endpoints were pharmacodynamics parameters, objective tumor response, and urinary pharmacodynamics markers of target inhibition. Between April 2019 and October 2021, 37 patients were enrolled in 3 US centers. No DLTs were observed in Part 1, and 0.72 mg/kg Nim equivalent was the dose selected for Part 2. In total, 52 TEAEs in 18 patients were CA102N-related; 4 (in 3 patients) were ≥ Grade 3. Exploratory analysis in the dose expansion cohort revealed a median progression-free survival of 3.7 (1.0, 6.77) months. Based on this study, CA102N as monotherapy or in combination with trifluridine-tipiracil, was safe and well-tolerated at the recommended Phase 2 dose of 0.72 mg/kg Nim equivalent in patients with locally advanced or metastatic solid tumors. Preliminary evidence of antitumor activity in CRC warrants further clinical development. (ClinicalTrials.gov registration number: NCT03616574. Registration date: August 6, 2018).

100 Deals associated with CA-102N

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic Colorectal Carcinoma	Phase 2	-	Holy Stone Healthcare Co., Ltd.	01 Jan 2024
Bladder Cancer	Preclinical	Taiwan Province	Holy Stone Healthcare Co., Ltd.	06 Sep 2024
Pancreatic Ductal Adenocarcinoma	Preclinical	Taiwan Province	Holy Stone Healthcare Co., Ltd.	06 Sep 2024
Triple Negative Breast Cancer	Preclinical	Taiwan Province	Holy Stone Healthcare Co., Ltd.	06 Sep 2024
Locally Advanced Malignant Solid Neoplasm	Discovery	United States	Holy Stone Healthcare Co., Ltd.	09 Apr 2019
Neoplasm Metastasis	Discovery	United States	Holy Stone Healthcare Co., Ltd.	09 Apr 2019