Delving into the Latest Updates on Lobaplatin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

DNA

Action

inhibitors

Mechanism

DNA inhibitors(DNA inhibitors), DNA alkylating agents

Therapeutic Areas

NeoplasmsHemic and Lymphatic DiseasesRespiratory Diseases+ [3]

Active Indication

Breast CancerLeukemiaSmall Cell Lung Cancer+ [2]

Inactive Indication-

Originator Organization-

Active Organization

Hainan Chang'an International Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC9H18N2O3Pt

InChIKeyRLXPIABKJFUYFG-UHFFFAOYSA-M

CAS Registry135558-11-1

AbstractTransarterial chemoembolization (TACE) utilizing a water‐in‐oil lipiodol emulsion is a preferable therapeutic strategy for advanced liver cancer in clinical practice. However, the low stability of the lipiodol emulsion and poor efficacy of chemotherapeutic drug seriously undermine the efficiency of TACE. Herein, a novel lobaplatin‐loaded lipiodol emulsion (denoted as ICN‐LPE) is developed by constructing a lipiodol Pickering emulsion (LPE) stabilized with iron‐doped carbon nanozymes (ICN) to mitigate the issue of lipiodol‐water separation. This novel emulsion not only solves the instability of conventional lipiodol emulsions, but also facilitates the sustained release of lobaplatin. More importantly, upon entry into tumor cells, ICN catalyze the generation of reactive oxygen species via the Fenton‐like reaction while simultaneously consuming intracellular glutathione, thereby inducing tumor cell death via chemodynamic therapy. By integrating chemotherapy and chemodynamic therapy, ICN‐LPE demonstrates a synergistic antitumor effect and effectively inhibits tumor growth in a rabbit liver tumor model. Therefore, our ICN‐LPE shows an appealing clinical application prospect for TACE.

29 Jan 2025·ACS Applied Materials & Interfaces

Supramolecular Combination Chemotherapy: Directly Inducing Immunogenic Cell Death To Inhibit Tumor Metastasis via Host–Guest Interactions

Article

Author: Liu, Qinye ; Sun, Xueting ; Wang, Yuanpeng ; Chen, Yueyue

Tumor metastasis is a difficult clinical problem to solve due to tumor heterogeneity and the emergence of antiapoptotic clones driven by tumor evolution. Clinical combination chemotherapy remains a standard treatment for solid metastasis tumors but with worse treatment efficiency. It is worth exploring a high-efficiency and low-side-effect therapeutic method to solve solid metastases. Herein, we fabricate a supramolecular combination chemotherapeutic system based on host-guest interactions using a cucurbit[8]uril complex (CB[8]-lobaplatin-oxaliplatin, CLO). We explored whether CLO can induce colorectal cancer cell death by activating immunogenic cell death (ICD) to inhibit cancer cell migration in a safe and effective manner. CLO inhibits the viability of human colorectal cancer cells (HCT116) at only 10 μM and alleviates the cytotoxicity induced by lobaplatin-oxaliplatin (LO) in normal colorectal cells (NCM460). Interestingly, CLO can trigger ICD in colorectal tumor cells, and our results verified the upregulations of high mobility group box 1 (HMGB1) and adenosine triphosphate (ATP) release and cell surface calreticulin (CRT) exposure. Besides, we found that CLO can inhibit tumor migration both in vivo and in vitro, and bio-AFM characterization of tumor cellular surface also confirmed this phenomenon. To further investigate the underlying mechanisms of the antitumor effects of CLO, quantitative proteomics was employed, and the results indicated that the citrate cycle (TCA cycle), protein processing in the endoplasmic reticulum, cGMP-PKG signaling pathway, p53 signaling pathway, chemical carcinogenesis, and necroptosis signaling pathway might contribute to CLO-induced antitumor effects. Collectively, our study suggests that the supramolecular combination chemotherapeutic system based on CB[8] host-guest complex can activate ICD to inhibit metastasis in antitumor strategy and exhibits a remarkable potential for supramolecular immunotherapy.

31 Dec 2024·Annals of Medicine

Lobaplatin-based concurrent chemoradiotherapy in elderly nasopharyngeal carcinoma

Article

Author: Zhou, Ping ; Yu, Yi-Feng ; Wu, San-Gang ; Zhou, Rui ; Lin, Qin

BACKGROUNDThe therapeutic benefit of concurrent chemoradiotherapy (CCRT) in elderly nasopharyngeal carcinoma (NPC) patients remains controversial. This study aimed to investigate the efficacy and toxicity of lobaplatin-based CCRT in elderly patients with NPC.METHODSWe included stage II-IVA NPC patients aged ≥65 years who received lobaplatin concomitant with intensity-modulated radiation therapy (IMRT) between March 2019 and January 2023. Objective response rates and treatment-related toxicity were assessed. Kaplan-Meier's analysis was performed to calculate survival rates.RESULTSA total of 29 patients were included with a median age of 67 years. There were 19 patients (65.5%) who had comorbidities. All patients had serum EBV-DNA detective before treatment; the median EBV-DNA load was 236 IU/mL. There were 25 (86.2%) patients treated with induction chemotherapy, and the overall response rate was 92.0%. All patients received IMRT and concurrent chemotherapy with lobaplatin. During the CCRT, the most common adverse effect was haematological toxicity. Three patients (10.3%) had grade 3 leucopenia, three patients (10.3%) had grade 3 neutropenia, and eight patients (27.6%) had grade 3-4 thrombocytopenia. The rate of grade 3 mucositis was 34.5%. No patients had liver and kidney dysfunction. The median weight loss was 4 kg during CCRT. After three months of CCRT, the total response rate was 100%. EBV-DNA was not detected in any patients. The median follow-up was 32.1 months. The 3-year locoregional recurrence-free survival, distant metastasis-free survival, progression-free survival and overall survival were 95.8%, 85.7%, 82.5% and 100%, respectively.CONCLUSIONSLobaplatin-based CCRT is safe and feasible for elderly NPC patients, with satisfactory short-term survival outcomes and acceptable toxicities. A phase 2 trial is ongoing to investigate the role of lobaplatin-based CCRT on long-term survival and treatment toxicities for this population.

100 Deals associated with Lobaplatin

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	L01XA	DB13049

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Breast Cancer	China	Hainan Chang'an International Pharmaceutical Co. Ltd.	-
Leukemia	China	Hainan Chang'an International Pharmaceutical Co. Ltd.	-
Small Cell Lung Cancer	China	Hainan Chang'an International Pharmaceutical Co. Ltd.	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Ovarian Epithelial Carcinoma	Phase 2	China	Hainan Chang'an International Pharmaceutical Co. Ltd.	30 May 2018
Platinum-sensitive epithelial ovarian cancer	Phase 2	China	Hainan Chang'an International Pharmaceutical Co. Ltd.	30 May 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06198465 (ESMO_IO2024) Manual	Phase 2	Gastroesophageal junction adenocarcinoma Neoadjuvant	15	Adebrelimab + nab-paclitaxel + lobaplatin + S-1	(wbbdwfskmy) = puifylqulr smkysjbkmv (wprmormwgk ) View more	Positive	12 Dec 2024
ChiCTR2100043027 (neoALTAL, ESMO 12023 \| ESMO 22023) Manual	Phase 2	Triple Negative Breast Cancer Neoadjuvant	45	Anlotinib + docetaxel+nab-paclitaxel + lobaplatin	(vjblzznder) = ghchezkwgx ekqjsoqtuw (krlzxafugd, 42.2 - 72.3) View more	Positive	21 Oct 2023
				Anlotinib + docetaxel+nab-paclitaxel + lobaplatin (IM subtype)	(vjblzznder) = keymgbchxe ekqjsoqtuw (krlzxafugd )
ASCO2023	Not Applicable	Nasopharyngeal Carcinoma Neoadjuvant	44	Tislelizumab and GP regimen	gamfzotcjm(anggflhnzx) = Grade 3-4 irAEs were rash(2) and hypothyroidism(1) rmvldxwkda (xiqxjjszfz )	Positive	31 May 2023
				Chemoradiotherapy including IMRT, lobaplatin and nimotuzumab
ChiCTR2100043027 (SWH-B006 (neoALTALL), SABCS2023)	Phase 2	Triple Negative Breast Cancer Neoadjuvant Ki-67 \| TP53 \| MYC ... View more	24	Anlotinib + Taxanes + Lobaplatin	lmrxddhhfz(dqezoemgdi) = whaajnkavq izjtskzdua (anhtczskrk, 36.6% - 77.9) View more	Positive	01 Mar 2023
Pubmed Manual	Not Applicable	Non-squamous non-small cell lung cancer Second line	126	Lobaplatin+Albumin-Bound Paclitaxel+Bevacizumab	(oudcjzxxyl) = bjbuckdypw ndrdjcoivg (taklbjatiq, 5.86 - 6.56) View more	Positive	26 Jun 2022
				Lobaplatin+Albumin-Bound Paclitaxel	(oudcjzxxyl) = mbtpvazspz ndrdjcoivg (taklbjatiq, 4.956 - 5.191) View more
NCT03057106 (CCTG BR34 \| CCTG BR.34, CTgov)	Phase 2	Metastatic Non-Squamous Non-Small Cell Lung Carcinoma	301	Tremelimumab+Durvalumab (Durvalumab and Tremelimumab)	(ozvutrdzgl) = pdtbywkews mxphqzgclk (rgtlwbkefg, eadlckpcth - shvcoqjezo) View more	-	09 Feb 2022
				Tremelimumab+Lobaplatin+Cisplatin,+Durvalumab+Nedaplatin (Platinum Based Chemotherapy + Durvalumab + Tremelimumab)	(ozvutrdzgl) = syfqjqcoaq mxphqzgclk (rgtlwbkefg, qrwnryuedx - qpeqpxyrjl) View more
NCT03413436 (Pubmed \| Front Oncol)	Phase 4	Esophageal Carcinoma Adjuvant	733	Lobaplatin plus docetaxel	idpmazylid(qcmrygtymj) = ksgsfbhlww clslbaukpq (yymotlrcpl ) View more	-	01 Jan 2021
				Cisplatin plus docetaxel	idpmazylid(qcmrygtymj) = atssdypbcx clslbaukpq (yymotlrcpl ) View more
CSCO2020	Not Applicable	Uterine Cervical Cancer	90	白蛋白紫杉醇联合洛铂经介入栓塞给药化疗	ulkpekspmh(ybsxqdplnt) = ctqcskhxso pxuzbeyxmx (fhbqswxvvg )	Positive	19 Sep 2020
NCT03188497 (Pubmed \| Transl Oncol)	Phase 1	Nasopharyngeal Carcinoma	17	Lobaplatin 25-50 mg/m2	(ffjjdeusyu) = hloeuafcfw xbeelsaknb (pilbwojxdi )	-	01 Aug 2018
ChiCTR-TRC-10001047 (ASCO2014)	Phase 3	Extensive stage Small Cell Lung Cancer First line	234	Lobaplatin/Etoposide	(ibdvekfooz) = ubilhzjzmr cjxndzcmuo (zczroynuya ) View more	-	20 May 2014
				Cisplatin/Etoposide	(ibdvekfooz) = umveemkfjj cjxndzcmuo (zczroynuya ) View more