Cipterbin (inetetamab)

The incidence of adverse events (AEs) was generally consistent across all levels. There were slight differences in the mean Cmax, Cmin, AUCtau and Cav between the three-week dosing group and the single-week dosing group, and the mean steady-state concentrations of Cav were comparable; however, there were no differences in efficacy, safety or immunogenicity between the two groups.

In the first-line treatment of HER2-positive advanced gastric cancer, inetetamab and trastuzumab showed comparable efficacy. The inetetamab group showed superior PFS, and both groups had good safety.

P4, N=200, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

For metastatic HER2-positive breast cancer patients with abnormal PAM pathway activation and previous trastuzumab treatment, the combination of inetetamab with sirolimus and chemotherapy is equivalent to the combination of pyrotinib and chemotherapy. Therefore, this regimen could be a treatment option for PAM pathway-activated metastatic HER2-positive breast cancer patients.

Due to its optimized antibody-dependent cell-mediated cytotoxicity effect compared with trastuzumab, it has shown good efficacy and safety in the treatment of HER2-positive advanced breast cancer (ABC)...Patients treated with inetetamab plus pyrotinib plus chemotherapy, especially with capecitabine, had the best outcomes (mPFS = 14.0 months)...Inetetamab-based combination therapy shows promising efficacy and good safety in patients with HER2-positive ABC. It is one of the late-line treatment options for Chinese patients with HER2-positive ABC.

P4, N=100, Not yet recruiting, Fudan University

Neoadjuvant therapy with TCbIP showed good efficacy and safety in patients with HER2-positive LABC and might be another promising option for neoadjuvant treatment.

To evaluate the efficacy and safety of a pyrotinib-based therapy for human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer (MBC) in the real world. Additionally, the concurrent administration of pyrotinib and inetetamab could be an alternative to consider in the second and higher-line treatment for metastatic breast cancer. The adverse reactions of pyrotinib were tolerable in general.

Human epidermal growth factor receptor 2 (HER2)-targeted agents have significantly improved the outcomes of patients with HER2-positive breast cancer; however, a large proportion of patients still develop resistance to trastuzumab. The combination regimen of inetetamab, pyrotinib, and oral vinorelbine showed encouraging efficacy and favorable safety in patients with HER2-positive advanced breast cancer and could be considered as an alternative treatment option for the patients. No.NCT05823623; https://www.clinicaltrials.gov/.

Inetetamab demonstrates effectiveness with a manageable safety profile, offering a promising therapeutic option for HER2-positive breast cancer patients who have shown resistance to prior anti-HER2 treatments.

P=N/A, N=40, Recruiting, Xi'an International Medical Center Hospital; Xi'an International Medical Center Hospital

Inetetamab and pyrotinib in combination with vinorelbine have good efficacy in ≥2ndline treatment of HER2-positive MBC with controllable toxicity, and the combination is a new treatment option, especially for patients who cannot use ADCs in 2nd-line treatment.

For the metastatic HER2 positive breast cancer patients with abnormal activation of PAM pathway treated with trastuzumab previously, the combination of inetetamab with sirolimus and chemotherapy regimen are equivalent to the combination of pyrotinib and chemotherapy regimen. It demonstrated that combination of inetetamab with sirolimus and chemotherapy could be one of the treatment options for the metastatic HER2 positive breast cancer patients.

No treatment-related serious adverse events or treatment-related deaths occurred. Conclusion The combination regimen of inetetamab combined with pyrotinib and vinorelbine showed an encouraging efficacy and favorable safety in patients with HER2 positive metastatic breast cancer.

Neoadjuvant therapy with TCbIP demonstrated promising efficacy and manageable toxicity in patients with HER2-positive locally advanced breast cancer. Registration number: NCT05749016 (www.clinicaltrials.gov).

Among them, 45 patients received second-line treatment who couldn't use T-DM1 or T-DXd, and 44 patients received ≥third-line treatment. Inetetamab + pyrotinib + vinorelbine demonstrates good efficacy and controllable toxicity as a second-line treatment for HER2-positive MBC. This therapeutic regimen provides a viable alternative option for patients who are unable to receive ADCs as the second-line treatment.

In this prospective, single-arm, phase 2 trial, patients with HER2-positive metastatic breast cancer after progression on trastuzumab were recruited. The combination regimen of inetetamab plus pyrotinib plus oral vinorelbine showed an encouraging efficacy and favorable safety in patients with HER2 positive metastatic breast cancer.

No treatment-related serious adverse events or treatment-related deaths occurred. Conclusions The combination regimen of inetetamab combined with pyrotinib and vinorelbine showed an encouraging efficacy and favorable safety in patients with HER2 -positive metastatic breast cancer.

P2, N=46, Active, not recruiting, Henan Cancer Hospital | Recruiting --> Active, not recruiting | Trial completion date: Oct 2022 --> Dec 2024

Moreover, inetetamab, an innovative anti-HER2 monoclonal antibody, has a more potent antibody-dependent cell-mediated cytotoxicity (ADCC)-inducing effect than trastuzumab, which has been shown to be an effective and rational strategy in the clinic when combined with multiple chemotherapeutic agents. In addition, cisplatin enhanced the PBMC-killing ability of inetetamab by inducing GSDMB-mediated pyroptosis, which can be explained by increased secretion of IFN-γ. Our study reveals that the anti-HER2 monoclonal antibody inetetamab may be an attractive candidate for LUAD therapy, which opens new avenues for therapeutic interventions for LUAD.

P2, N=30, Recruiting, The First Affiliated Hospital with Nanjing Medical University | Initiation date: Sep 2022 --> Feb 2022

P=N/A, N=150, Not yet recruiting, Hunan Cancer Hospital

Conclusions Inetetamab plus pyrotinib and utidelone may be an excellent scheme for HER2-positive metastatic breast cancer. This trial is still ongoing and needs long-term follow-up.

Among them, 45 patients received second-line treatment who couldn't use T-DM1 or T-DXd, and 44 patients received ≥third-line treatment. Conclusions The VIP regimen demonstrated good efficacy and controllable toxicity as a second-line treatment for HER2-positive MBC. This therapeutic regimen provides a viable alternative option for patients who are unable to receive ADCs as the second-line treatment.

No significant reduction in the left ventricular ejection fraction was observed in any patient. Conclusions Neoadjuvant therapy with TCbIP has shown promising efficacy and manageable toxicity in patients with HER2-positive LA breast cancer.

HER2+ MBC patients pretreated with multiple-line therapies still respond to inetetamab-based treatment. Inetetamab combined with vinorelbine and pyrotinib may be the most effective treatment regimen, with a controllable and tolerable safety profile.

P=N/A, N=100, Recruiting, Zhejiang Cancer Hospital

TCbIP displays a promising efficacy (pCR rate of 66.7%) and manageable toxicity in patients with HER2-positive LA breast cancer in the neoadjuvant setting. Clinical trial information: NCT05749016.

The preliminary data of inetetamab in combination with pyrotinib showed manageable safety and compelling antitumor activity in advanced NSCLC patients harboring HER2 mutations. Clinical trial information: NCT05016544. >

P2, N=30, Recruiting, The First Affiliated Hospital with Nanjing Medical University

P=N/A, N=100, Recruiting, The First Affiliated Hospital with Nanjing Medical University | Trial completion date: Mar 2023 --> Mar 2024 | Trial primary completion date: Mar 2023 --> Mar 2024

P=N/A, N=100, Recruiting, The First Affiliated Hospital with Nanjing Medical University

P2, N=30, Recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences

Although the combination of trastuzumab with pertuzumab produced synergetic effects in the treatment of HER2-overexpressing cancers, not all patients with HER2 overexpression benefited from the trastuzumab plus pertuzumab combination. We showed that pan-TKIs-induced synergistic antitumor effects with inetetamab in the treatment of these two types of cancers and that adding chemotherapeutic agents to the existing TKI plus anti-HER2 monoclonal antibody combination strategies induced additional inhibitory effects, suggesting that such combination strategies may be choices for the treatment of these two tumors. Thus, combination therapies targeting distinct and broad pathways that are essential for tumor growth and survival can be effective for treating metastatic breast cancers and gastric cancers.

Background: The HER2-targeted drugs selection after trastuzumab failure has become a challenging issue for HER2-positive metastatic breast cancer (MBC) patients. Inetetamab combined with pyrotinib and chemotherapy showed a promising efficacy and a good tolerance in patients with HER2-positive metastatic breast cancer, confirming the synergistic effect between the ADCC optimized monoclonal antibodies and TKIs, which brings more treatment options for HER2- positive metastatic breast cancer.

P2, N=46, Recruiting, Henan Cancer Hospital | Trial primary completion date: Apr 2022 --> Nov 2021

P2, N=120, Recruiting, Henan Cancer Hospital | Not yet recruiting --> Recruiting

P2, N=120, Not yet recruiting, Henan Cancer Hospital

P4, N=70, Not yet recruiting, Chinese Academy of Medical Sciences

P4, N=60, Recruiting, Zhejiang Cancer Hospital

P2, N=46, Recruiting, Henan Cancer Hospital | Not yet recruiting --> Recruiting

P1/2, N=48, Recruiting, Sun Yat-sen University