Leronlimab(Leronlimab) - 药物靶点：CCR5_在研适应症：转移性结直肠癌，微卫星稳定型结直肠癌，不能切除的大肠癌_专利_临床

概要

基本信息

药物类型

单克隆抗体

别名

Leronlimab (USAN/INN)、Leronlimab-PRO 140、leronlimab-PRO140

+ [6]

靶点

CCR5

作用方式

拮抗剂

作用机制

CCR5拮抗剂(C-C趋化因子受体5型拮抗剂)

治疗领域

肿瘤消化系统疾病神经系统疾病+ [1]

在研适应症

转移性结直肠癌微卫星稳定型结直肠癌不能切除的大肠癌+ [2]

非在研适应症

急性移植物抗宿主病急性髓性白血病新型冠状病毒感染+ [6]

原研机构

CytoDyn, Inc.

在研机构

CytoDyn, Inc.

非在研机构-

权益机构

The American Foundation For AIDS Research, Inc.

BIOMM SA

MacLeods Pharmaceuticals Ltd.

+ [8]

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)、紧急使用授权 (加拿大)、快速通道 (美国)

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结构/序列

Sequence Code 651154043H

来源: *****

Sequence Code 651154044L

来源: *****

关联

27

项与 Leronlimab 相关的临床试验

NCT06699836

/ Recruiting临床2期

A Phase Two Study Evaluating Two Doses of Leronlimab (PRO 140) In Combination With Trifluridine + Tipiracil (TAS-102) + Bevacizumab in Participants With Microsatellite Stable (MSS), Relapsed Refractory Metastatic Colorectal Cancer (mCRC)

This is an open label, randomized, two arm, multi-center study to explore the effect of leronlimab on the overall response rate/ overall survival and safety and tolerability when used in combination with trifluridine and tipiracil + bevacizumab in patients with MSS, mCRC who have progressed on prior treatment before participating in the study. The main questions this study aims to answer are:
1. Can leronlimab, in combination with standard of care therapies trifluridine and tipiracil+ bevacizumab, increase the objective response rate in persons with MSS, mCRC who have progressed on prior treatment before participating in the study.
2. Is leronlimab safe and well tolerated in these subjects when used in combination with standard of care therapies trifluridine and tipiracil+ bevacizumab.

开始日期2025-06-16

申办/合作机构

CytoDyn, Inc.

[+1]

NCT05730673

/ Withdrawn临床2期

A Phase II Study of Leronlimab (PRO 140) in Combination With Regorafenib in Patients With CCR5+, Microsatellite Stable (MSS), Metastatic Colorectal Cancer (mCRC)

This is aPhase II Study of Leronlimab (PRO 140) in combination with Regorafenib in Patients with CCR5+, Microsatellite Stable (MSS), Metastatic Colorectal Cancer (mCRC)

开始日期2022-09-20

申办/合作机构

CytoDyn, Inc.

[+1]

NCT04901689

/ Suspended临床3期IIT

A Phase 3, Randomized, Double Blind, Placebo Controlled Trial to Evaluate the Efficacy and Safety of Leronlimab in Combination With Standard of Care for Patients With Coronavirus Disease 2019 (COVID-19) With Need for Mechanical Ventilation or Extracorporeal Membrane Oxygenation

Leronlimab (PRO 140) is a humanized IgG4,k monoclonal antibody (mAb) that recognizes the C-C chemokine receptor type 5 (CCR5). Disruption of the C-C chemokine ligand 5 (CCL5)-CCR5 axis via leronlimab-mediated CCR5 blockade might prevent pulmonary trafficking of pro-inflammatory leukocytes and dampen pathogenic immune activation in coronavirus disease 2019 (COVID-19).
The purpose of the study is to assess the safety and efficacy of leronlimab plus standard of care in critically ill patients hospitalized with COVID-19 pneumonia who are requiring mechanical ventilation or extracorporeal oxigenation (ECMO).

开始日期2021-10-23

申办/合作机构

Hospital Israelita Albert Einstein

[+1]

100 项与 Leronlimab 相关的临床结果

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100 项与 Leronlimab 相关的转化医学

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100 项与 Leronlimab 相关的专利（医药）

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71

项与 Leronlimab 相关的文献（医药）

2025-09-01·JOURNAL OF MOLECULAR MODELING

Quantum chemical calculations based on 4,5-di(1,2,4-oxadiazol-3-yl)-2H-1,2,3-triazole and 3,3′ -(2H-1,2,3-triazole-4,5-diyl)-bis(1,2,4-oxadiazol-5(4H)-one) derivatives: a DFT study

Article

作者: Zhang, Peng ; Ma, Peng ; Chu, YuQin ; Ma, CongMing ; Zhu, Yang ; Jiang, Wen

CONTEXT:

1,2,3-Triazole has excellent thermal stability, and both 1,2,3-triazole and 1,2,4-oxazolium are good in structural modifiability. This study employed density functional theory (DFT) to design 24 target compounds (designated PA-1 to PA-24) based on the characteristics of these two heterocyclic systems. Using 4,5-diallyl-2H-1,2,3-triazole-3,3'-(2H-1,2,3-triazole-4,5-diyl)-bis(1,2,4-oxadiazol-5(4H)-one) as the parent compound (labeled A1), we introduced different energetic substituents at the C3 position of the oxadiazole ring and the N2 position of the triazole ring. Alternatively, using 3,3'-(2H-1,2,3-triazole-4,5-diyl)-bis(1,2,4-oxadiazol-5(4H)-one) as the parent compound (labeled A2), we introduced different energetic substituents at the N2 position of the triazole ring. The selection process considered both macroscopic properties (heat of formation and detonation performance) and microscopic factors including frontier molecular orbitals, energy gaps, weak interactions, surface electrostatic potential, and bond parameters. This approach aimed to identify energetic materials with both detonation performance and safety characteristics while investigating how introducing different substituents at these two positions affects detonation performance and safety. The research results indicate the following: First, introducing an azide group at the C3 position of the oxadiazole in A1 more effectively enhances the compound's heat of formation. PA-13 (△H_f,sold = 972.97 kJ/mol), PA-14 (△H_f,sold = 1023.62 kJ/mol), and PA-15 (△H_f,sold = 1069.24 kJ/mol), which all contain azide groups, rank among the top three in heat of formation among the 24 compounds. Second, PA-6 (D = 9.31 km/s, P = 39.93 GPa, Q = 7.39 kJ/g) exhibits the best detonation performance: its detonation pressure exceeds those of RDX (G = 36GPa), its detonation velocity and detonation heat surpass that of HMX (D = 9 km/s, Q = 6.4 kJ/g), and it achieves the ideal state of zero oxygen balance, resulting in the highest energy utilization efficiency. Third, PA-19 showed the least impact sensitivity and showed the potential of an insensitive explosive. Fourth, hydrogen bonds are common in the molecular structure of PA-8 ~ PA-12 derivatives of A2, which may contribute to the stability of the molecules. Fifth, trinitromethyl and dinitromethyl groups are more prone to fragmentation. The substituents introduced at the C3 position of the oxadiazole have almost no effect on the ring length of the oxadiazole, but introducing trinitromethyl at the N2 position of the triazole causes the triazole ring structure to expand, resulting in an increased ring length.

METHOD:

All calculations in this paper are based on density functional theory and were performed using the Gaussian16 software. Initially, the structures of PA-1 to PA-24 were optimized at the B3LYP-D3/6-311G** level. Subsequently, single-point energy calculations were conducted at the M06-2X-D3/def2-TZVPP level to determine the formation enthalpy, detonation velocity, and detonation pressure of the compounds. The Multiwfn and VMD programs were used to plot the energy gap diagrams, isosurface maps, scatter plots, and surface electrostatic potential maps for PA-1 to PA-24.

2025-08-01·INFLAMMOPHARMACOLOGY

Chemokine receptor type-5: a key regulator of immunity, disease pathogenesis, and emerging therapeutic target

Review

作者: Vanaja, Kenchappa ; Bambal, Vaishali ; Kodihalli Basavaraj, Priyanka

CCR5 (C-C chemokine receptor type 5) is a critical chemokine receptor involved in immune cell migration, signaling, and inflammation. Expressed on T lymphocytes, macrophages, and dendritic cells, it regulates leukocyte recruitment to inflamed sites via ligands such as CCL3, CCL4, and CCL5. Beyond immune regulation, CCR5 is implicated in diseases like rheumatoid arthritis, inflammatory bowel disease, and atherosclerosis, where the CCL5/CCR5 axis exacerbates inflammation and tissue damage. In cancer, CCR5 promotes tumor growth, metastasis, and immune evasion, particularly in aggressive breast cancer subtypes (basal and HER-2 +). It also serves as a co-receptor for HIV entry, with the CCR5Δ32 mutation conferring resistance. With therapeutic inhibition of CCR5 gaining attention, Maraviroc is approved for HIV treatment, while monoclonal antibodies such as leronlimab, genetic strategies (CRISPR), and dual CCR2/CCR5 antagonists such as cenicriviroc are under investigation for broader applications. Blocking CCR5 has shown efficacy in reducing metastasis and improving chemotherapy outcomes, reinforcing its therapeutic potential. Along with CCR5's role in disease pathogenesis, emphasizing its involvement in immune regulation and inflammatory processes, this review explores the multifaceted role of CCR5 in immunity, its contribution to disease pathogenesis, and innovative therapeutic interventions targeting CCR5 to modulate immune responses and treat diseases.

2025-06-01·JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Leronlimab Treatment for Multidrug-Resistant HIV-1 (OPTIMIZE): A Randomized, Double-Blind, Placebo-Controlled Trial

Article

作者: Hansen, Scott G. ; Dejesus, Edwin ; Sanchez, William E. ; Gathe, Joseph C. ; Meidling, Joseph ; Lalezari, Jacob P. ; Sacha, Jonah B. ; Krishen, Alok ; Ramgopal, Moti N. ; Rolle, Charlotte-Paige ; Yang, Otto O.

Background::

Leronlimab is a humanized κ-IgG4 monoclonal antibody that blocks C–C chemokine receptor type 5. We investigated leronlimab as a treatment option for people living with multidrug-resistant HIV-1.

Setting and Methods::

In a phase 2b/3, multicenter, randomized, double-blind, placebo-controlled study conducted in 21 hospital centers in the United States, treatment-experienced people living with HIV with documented drug resistance were randomly assigned once weekly leronlimab (350 mg subcutaneously) or matching placebo for 1 week overlapping existing failing antiretroviral therapy, followed by a 24-week single-arm extension with weekly leronlimab combined with a new optimized background treatment. The primary end point was achieving ≥0.5 log10 reduction in plasma HIV-1 RNA from baseline at the end of the 1-week double-blinded treatment period.

Results::

Fifty-two participants were enrolled (25 leronlimab and 27 placebo). After the 1-week randomized phase, by the intent-to-treat analysis, 64.0% (16/25) receiving leronlimab achieved ≥0.5 log10 reduction in plasma HIV-1 RNA versus 23.1% (6/26) receiving placebo (P = 0.0032), whereas by per protocol analysis, 72.7% (16/22) receiving leronlimab achieved ≥0.5 log10 reduction in plasma HIV-1 RNA versus 24.0% (6/25) receiving placebo (P = 0.0008). Leronlimab was generally well tolerated with no drug-related serious adverse events reported. Overall, 175 adverse events were reported by 34/52 participants, with 120 (68.6%) adverse events categorized as mild.

Conclusions::

Leronlimab resulted in significantly reduced plasma HIV-1 within 1 week after addition to failing antiretroviral therapy. After 24 weeks combined with an optimized background treatment, most participants had plasma HIV-1 RNA levels <50 copies per milliliter plasma, suggesting utility of leronlimab as a component of salvage therapy.

183

项与 Leronlimab 相关的新闻（医药）

2026-04-14

·BioSpace

CytoDyn to Present at the AACR Annual Meeting 2026

VANCOUVER, Wash., April 14, 2026 (GLOBE NEWSWIRE) -- CytoDyn Inc. (OTCQB: CYDY) ("CytoDyn" or the "Company"), a clinical-stage oncology company advancing leronlimab, a first-in-class humanized monoclonal antibody targeting the CCR5 receptor with therapeutic potential across multiple indications, including metastatic triple-negative breast cancer (“mTNBC”) and colorectal cancer (“mCRC”), today announced that it will be presenting two posters at the American Association for Cancer Research (AACR) Annual Meeting 2026, taking place April 17–22, 2026, in San Diego, California. Details of the poster presentations are as follows: Abstract title: Leronlimab induces PD-L1 expression and is associated with long term survival with an ICI in PD-L1 low metastatic TNBC Presenter: Richard Pestell, M.D., Ph.D., FRCP AO, Lead Consultant in Preclinical and Clinical Oncology at CytoDyn Date and Time: April 19, 2026, from 2:00 p.m. – 5:00 p.m. PST. Poster ID: 1033 Location: Section 41, Board 1 Abstract title: Preliminary results of a phase 2 study of leronlimab in combination with TAS-102 and bevacizumab in previously treated metastatic colorectal cancer Presenter: Pashtoon M. Kasi, M.D., M.S., Medical Director at City of Hope Date and Time: April 21, 2026, from 2:00 p.m. – 5:00 p.m. PST. Poster ID: 6466 Location: Section 41, Board 14 “We are encouraged by the continued progress being made as we advance leronlimab and explore its potential applications across solid tumors,” said Jacob Lalezari, M.D., CEO of CytoDyn. “The research being presented at AACR reflects the growing body of scientific work examining CCR5 biology and its role in the tumor microenvironment. Together, these studies help deepen our understanding of how leronlimab may enhance immune responses and inform our broader strategy to develop new treatment approaches for patients with difficult-to-treat cancers.” A copy of the presentations will be made available on CytoDyn’s website under the Publications & Posters section after it is presented at the symposium. About CytoDyn CytoDyn is a clinical-stage oncology company dedicated to advancing leronlimab, a first-in-class humanized monoclonal antibody that targets the CCR5 receptor, a key regulator of immune function implicated in cancer, infectious diseases, and autoimmune disorders. Guided by a mission to improve patients’ quality of life through therapeutic innovation, CytoDyn is committed to integrity, responsibility, and service as it works to bring transformative treatments to patients worldwide. For more information, please visit and follow us on LinkedIn . Note Regarding Forward-Looking Statements This news release may contain forward-looking statements relating to, among other things, the mechanism of action of leronlimab, clinical trial results, product development, market position, future operating and financial performance, and business strategy. The reader is cautioned not to rely on these statements, which are based on current expectations of future events. For important information about these statements and our Company, including the risks, uncertainties and other factors that could cause actual results to vary materially from the assumptions, expectations and projections expressed in any forward-looking statements, the reader should review our Annual Report on Form 10-K for the fiscal year ended May 31, 2025, including the section captioned “Forward-Looking Statements” and in Item 1A, as well as subsequent reports filed with the Securities and Exchange Commission. CytoDyn Inc. does not undertake to update any forward-looking statement as a result of new information or future events or developments except as required by applicable law. Corporate Contact CytoDyn Inc. ir@cytodyn.com Media Contacts David Schull or Ignacio Guerrero-Ros, Ph.D. Russo Partners, LLC CytoDyn@russopartnersllc.com

临床2期临床结果AACR会议ASCO会议

2026-03-31

·百度百家

「AACR 2026」GPCR靶点盘点：从CXCR4到GPRC5D，哪些方向正在走热？

在肿瘤创新药研发中，G蛋白偶联受体（GPCR）一直是一个有些尴尬的靶点家族。从成药史来看，它是最成熟的一类药物靶点；但从肿瘤新药版图来看，GPCR又长期没有HER2、TROP2、CLDN18.2这类靶点那么显眼。不过，从AACR 2026的摘要趋势来看，这种局面正在发生变化。本届会议上，GPCR相关项目已经明显从传统小分子受体调控，延伸到肿瘤微环境、Treg清除、ADC、双抗、多特异性分子以及放射性药物等多个方向。尤其是CXCR4、SSTR2、CCR8、LGR5、GPRC5D、CCR5等靶点，不仅摘要露出相对集中，而且已经出现较清晰的产品化和平台化开发路径。 1、CXCR4：成熟靶点仍在迭代，转移与微环境价值持续放大在GPCR靶点中，CXCR4依然是最成熟、也最接近临床转化的一类。它在肿瘤中的价值主要围绕细胞迁移、骨髓归巢、转移、耐药和微环境重塑展开，因此既有基础研究深度，也有较强的临床延展性。AACR 2026上，CXCR4的关注点已经从“做不做这个靶点”进一步转向为“如何做患者分层、如何进入联合治疗，以及如何挖掘更明确的应答人群”。从本届摘要来看，CXCR4方向既有Motixafortide这类明确分子的临床转化信号，也有TNX-1700这样的新项目线索，说明这一靶点仍然处于持续活跃状态。代表性摘要包括： CXCR4作用机制及药物研究进展 2、SSTR2：从核药标杆靶点，走向更广义的偶联平台靶点在GPCR家族中，SSTR2是最具“核药属性”的代表靶点之一。过去提到SSTR2，首先想到的通常是神经内分泌肿瘤和放射配体治疗；但AACR 2026显示，这个靶点的开发边界正在快速拓宽，已经不再局限于传统的显像或核素治疗，而是明显延伸到肽偶联药物、双特异性ADC以及新型放射性偶联药物。从布局主体看，Italfarmaco、基石药业、上海核舟医药都带来了明确项目线索，说明SSTR2正在从“经典核药靶点”逐步演变成一个更广义的偶联递送平台靶点。代表性摘要包括： 3、CCR8：Treg清除赛道持续升温，免疫抑制微环境成为核心切口如果说本届AACR上哪个GPCR靶点最能体现“肿瘤免疫新方向”，那CCR8一定是重点之一。CCR8与肿瘤浸润性调节性T细胞（Treg）高度相关，因此天然适合作为肿瘤免疫抑制微环境改造的切入点。相比传统免疫激活逻辑，CCR8更强调定向清除肿瘤相关Treg，这也是它快速升温的重要原因。从今年AACR的摘要看，CCR8已经出现较完整的开发梯队：既有去除型抗体的分子特征研究，也有一期临床结果，甚至开始向ADC方向延展。布局主体包括Kainova Therapeutics、Amgen、Takeda，产业化信号已经比较明确。代表性摘要包括： 4、LGR5：从肿瘤干细胞标志物，走向ADC与双抗开发靶点 LGR5是一个典型的“生物学意义先行、药物开发逐步跟上”的靶点。它长期与肿瘤干细胞、耐药和复发相关，因此早年更多出现在机制研究中。但从AACR 2026的信号来看，LGR5正在快速摆脱“只适合做文章”的印象，转向更实在的抗体药物开发阶段。这次会议里，LGR5方向已经出现LGR5靶向ADC、EGFRxLGR5双抗、VHH抗体等多种策略，说明它正在成为实体瘤中值得重新评估的可药物化靶点。企业层面，Dragon Boat Biopharmaceutical的项目推进最为直接。代表性摘要包括： 5、GPRC5D：骨髓瘤赛道里最具热度的GPCR靶点之一在血液瘤领域，GPRC5D已经成为继BCMA之后极具关注度的新一代靶点之一。尤其是在多发性骨髓瘤中，GPRC5D为复发难治患者提供了新的靶向维度，也因此成为多特异性抗体和T-cell engager开发中的重点对象。AACR 2026上，这一靶点已经不再只是概念验证，而是明显进入了平台竞争与分子设计优化阶段。从摘要看，GPRC5D方向既有Talquetamab相关临床应用背景，也有多特异性抗体和多价多特异性ADC的新设计。相关布局主体包括Integral Molecular和Synthetic Design Lab，显示这一靶点正在进入“谁能做得更优”的竞争阶段。代表性摘要包括： 6、CCR5：老靶点正在被重新激活，联合治疗价值值得重估和前面几个靶点相比，CCR5并不是一个“新方向”。它在炎症、病毒感染和免疫迁移领域早已被广泛研究，因此很多人对它的第一印象甚至不是肿瘤。但AACR 2026的一些摘要提示，CCR5在肿瘤中的开发空间远未被挖尽，尤其是在联合治疗、微环境调控和适应症拓展上仍有不少机会。这次会议中，CCR5相关线索主要围绕leronlimab和maraviroc等已有分子的再利用展开，体现出典型的“老靶点新场景”特征。对于希望寻找机制成熟、转化路径相对清晰的团队来说，CCR5仍然值得持续关注。代表性摘要包括： 7、CXCR2：肿瘤炎症轴的关键节点，适合与免疫和微环境策略联动在本届AACR中，CXCR2的摘要数量不算最多，但研究方向非常集中，几乎都围绕IL-8、中性粒细胞募集、肿瘤炎症和休眠细胞唤醒展开。这类靶点的价值不在于单纯作用于肿瘤细胞，而在于它连接了肿瘤与髓系免疫系统之间的通讯网络，因此很适合与免疫治疗、炎症阻断和耐药微环境调控联动。从企业化线索看，虽然本次会议上披露的成熟项目不算多，但AZD5069等已有分子仍然给出了较明确的转化方向。代表性摘要包括： 8、DRD1：神经递质受体在肿瘤中的角色，正从边缘走向前沿如果说前面的几个靶点已经更接近“产品开发逻辑”，那么DRD1更像是本届AACR中一个值得前瞻关注的信号。作为多巴胺受体家族成员，DRD1传统上并不属于肿瘤药物开发的核心靶点，但这次多篇摘要将其与EZH2、表观遗传调控和三阴性乳腺癌进展联系起来，提示神经递质信号和肿瘤表观遗传之间的交叉正在被重新认识。目前这一方向仍以前沿研究为主，产业化布局还不密集，但恰恰因为处于早期，更值得被持续跟踪。代表性摘要包括：回看AACR 2026，可以非常明显地感受到，GPCR已经不再只是传统小分子药物的主场。在肿瘤领域，越来越多的GPCR靶点正在进入抗体、ADC、双抗、放射性药物和免疫微环境重塑的开发体系。其中，CXCR4、CCR8、CCR5、CXCR2更偏向免疫与微环境调控；SSTR2代表的是核药与偶联药物的持续融合；而LGR5、GPRC5D则更像是GPCR靶点走向抗体工程、多特异性分子和ADC开发的标志性案例。如果说过去行业对GPCR的判断还是“肿瘤里有机会，但不算主流”，那么从今年AACR的趋势看，至少一部分GPCR靶点，已经开始真正进入主流创新药视野。

2026-03-31

·有驾

「AACR 2026」GPCR靶点盘点：从CXCR4到GPRC5D，哪些方向正在走热？

在肿瘤创新药研发中，G蛋白偶联受体（GPCR）一直是一个有些尴尬的靶点家族。从成药史来看，它是最成熟的一类药物靶点；但从肿瘤新药版图来看，GPCR又长期没有HER2、TROP2、CLDN18.2这类靶点那么显眼。不过，从AACR 2026的摘要趋势来看，这种局面正在发生变化。本届会议上，GPCR相关项目已经明显从传统小分子受体调控，延伸到肿瘤微环境、Treg清除、ADC、双抗、多特异性分子以及放射性药物等多个方向。尤其是CXCR4、SSTR2、CCR8、LGR5、GPRC5D、CCR5等靶点，不仅摘要露出相对集中，而且已经出现较清晰的产品化和平台化开发路径。 1、CXCR4：成熟靶点仍在迭代，转移与微环境价值持续放大在GPCR靶点中，CXCR4依然是最成熟、也最接近临床转化的一类。它在肿瘤中的价值主要围绕细胞迁移、骨髓归巢、转移、耐药和微环境重塑展开，因此既有基础研究深度，也有较强的临床延展性。AACR 2026上，CXCR4的关注点已经从“做不做这个靶点”进一步转向为“如何做患者分层、如何进入联合治疗，以及如何挖掘更明确的应答人群”。从本届摘要来看，CXCR4方向既有Motixafortide这类明确分子的临床转化信号，也有TNX-1700这样的新项目线索，说明这一靶点仍然处于持续活跃状态。代表性摘要包括： CXCR4作用机制及药物研究进展 2、SSTR2：从核药标杆靶点，走向更广义的偶联平台靶点在GPCR家族中，SSTR2是最具“核药属性”的代表靶点之一。过去提到SSTR2，首先想到的通常是神经内分泌肿瘤和放射配体治疗；但AACR 2026显示，这个靶点的开发边界正在快速拓宽，已经不再局限于传统的显像或核素治疗，而是明显延伸到肽偶联药物、双特异性ADC以及新型放射性偶联药物。从布局主体看，Italfarmaco、基石药业、上海核舟医药都带来了明确项目线索，说明SSTR2正在从“经典核药靶点”逐步演变成一个更广义的偶联递送平台靶点。代表性摘要包括： 3、CCR8：Treg清除赛道持续升温，免疫抑制微环境成为核心切口如果说本届AACR上哪个GPCR靶点最能体现“肿瘤免疫新方向”，那CCR8一定是重点之一。CCR8与肿瘤浸润性调节性T细胞（Treg）高度相关，因此天然适合作为肿瘤免疫抑制微环境改造的切入点。相比传统免疫激活逻辑，CCR8更强调定向清除肿瘤相关Treg，这也是它快速升温的重要原因。从今年AACR的摘要看，CCR8已经出现较完整的开发梯队：既有去除型抗体的分子特征研究，也有一期临床结果，甚至开始向ADC方向延展。布局主体包括Kainova Therapeutics、Amgen、Takeda，产业化信号已经比较明确。代表性摘要包括： 4、LGR5：从肿瘤干细胞标志物，走向ADC与双抗开发靶点 LGR5是一个典型的“生物学意义先行、药物开发逐步跟上”的靶点。它长期与肿瘤干细胞、耐药和复发相关，因此早年更多出现在机制研究中。但从AACR 2026的信号来看，LGR5正在快速摆脱“只适合做文章”的印象，转向更实在的抗体药物开发阶段。这次会议里，LGR5方向已经出现LGR5靶向ADC、EGFRxLGR5双抗、VHH抗体等多种策略，说明它正在成为实体瘤中值得重新评估的可药物化靶点。企业层面，Dragon Boat Biopharmaceutical的项目推进最为直接。代表性摘要包括： 5、GPRC5D：骨髓瘤赛道里最具热度的GPCR靶点之一在血液瘤领域，GPRC5D已经成为继BCMA之后极具关注度的新一代靶点之一。尤其是在多发性骨髓瘤中，GPRC5D为复发难治患者提供了新的靶向维度，也因此成为多特异性抗体和T-cell engager开发中的重点对象。AACR 2026上，这一靶点已经不再只是概念验证，而是明显进入了平台竞争与分子设计优化阶段。从摘要看，GPRC5D方向既有Talquetamab相关临床应用背景，也有多特异性抗体和多价多特异性ADC的新设计。相关布局主体包括Integral Molecular和Synthetic Design Lab，显示这一靶点正在进入“谁能做得更优”的竞争阶段。代表性摘要包括： 6、CCR5：老靶点正在被重新激活，联合治疗价值值得重估和前面几个靶点相比，CCR5并不是一个“新方向”。它在炎症、病毒感染和免疫迁移领域早已被广泛研究，因此很多人对它的第一印象甚至不是肿瘤。但AACR 2026的一些摘要提示，CCR5在肿瘤中的开发空间远未被挖尽，尤其是在联合治疗、微环境调控和适应症拓展上仍有不少机会。这次会议中，CCR5相关线索主要围绕leronlimab和maraviroc等已有分子的再利用展开，体现出典型的“老靶点新场景”特征。对于希望寻找机制成熟、转化路径相对清晰的团队来说，CCR5仍然值得持续关注。代表性摘要包括： 7、CXCR2：肿瘤炎症轴的关键节点，适合与免疫和微环境策略联动在本届AACR中，CXCR2的摘要数量不算最多，但研究方向非常集中，几乎都围绕IL-8、中性粒细胞募集、肿瘤炎症和休眠细胞唤醒展开。这类靶点的价值不在于单纯作用于肿瘤细胞，而在于它连接了肿瘤与髓系免疫系统之间的通讯网络，因此很适合与免疫治疗、炎症阻断和耐药微环境调控联动。从企业化线索看，虽然本次会议上披露的成熟项目不算多，但AZD5069等已有分子仍然给出了较明确的转化方向。代表性摘要包括： 8、DRD1：神经递质受体在肿瘤中的角色，正从边缘走向前沿如果说前面的几个靶点已经更接近“产品开发逻辑”，那么DRD1更像是本届AACR中一个值得前瞻关注的信号。作为多巴胺受体家族成员，DRD1传统上并不属于肿瘤药物开发的核心靶点，但这次多篇摘要将其与EZH2、表观遗传调控和三阴性乳腺癌进展联系起来，提示神经递质信号和肿瘤表观遗传之间的交叉正在被重新认识。目前这一方向仍以前沿研究为主，产业化布局还不密集，但恰恰因为处于早期，更值得被持续跟踪。代表性摘要包括：回看AACR 2026，可以非常明显地感受到，GPCR已经不再只是传统小分子药物的主场。在肿瘤领域，越来越多的GPCR靶点正在进入抗体、ADC、双抗、放射性药物和免疫微环境重塑的开发体系。其中，CXCR4、CCR8、CCR5、CXCR2更偏向免疫与微环境调控；SSTR2代表的是核药与偶联药物的持续融合；而LGR5、GPRC5D则更像是GPCR靶点走向抗体工程、多特异性分子和ADC开发的标志性案例。如果说过去行业对GPCR的判断还是“肿瘤里有机会，但不算主流”，那么从今年AACR的趋势看，至少一部分GPCR靶点，已经开始真正进入主流创新药视野。

100 项与 Leronlimab 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11399	Leronlimab	-	DB05941

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
HIV感染	申请上市	美国	CytoDyn, Inc.	2021-11-01
新型冠状病毒感染	临床3期	美国	CytoDyn, Inc.	2020-08-05
不能切除的大肠癌	临床2期	美国	CytoDyn, Inc.	2025-06-16
转移性结直肠癌	临床2期	-	CytoDyn, Inc.	2022-09-20
转移性微卫星稳定结直肠癌	临床2期	-	CytoDyn, Inc.	2022-09-20
微卫星稳定型结直肠癌	临床2期	-	CytoDyn, Inc.	2022-09-20
新冠肺炎后遗症	临床2期	美国	CytoDyn, Inc.	2021-03-01
代谢功能障碍相关脂肪性肝炎	临床2期	美国	CytoDyn, Inc.	2020-12-01
转移性实体瘤	临床2期	美国	CytoDyn, Inc.	2020-05-01
三阴性乳腺癌	临床2期	美国	CytoDyn, Inc.	2019-04-22

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02859961 (CTgov)	临床2/3期	HIV感染	562	PRO 140 (Part 1 - 350 mg Weekly Injections of PRO 140, Group A)	鑰艱餘網膚壓鑰襯窪蓋 = 範衊膚鑰壓選淵蓋夢願醖憲窪製範構齋夢鹹醖 (顧願齋艱醖淵淵廠鬱襯, 鬱襯廠觸淵窪壓鬱鏇醖 ~ 製壓構憲艱壓顧憲衊築) 更多	-	2026-03-04
				PRO 140 (Part 1 - 525 mg Weekly Injections of PRO 140, Group B)	鑰艱餘網膚壓鑰襯窪蓋 = 遞遞網獵選顧壓繭選夢醖憲窪製範構齋夢鹹醖 (顧願齋艱醖淵淵廠鬱襯, 壓築製願願網窪壓遞繭 ~ 觸餘鑰窪衊繭繭醖願鏇) 更多
NCT04504942 (Phase 2 single-arm basket study, CTgov)	临床2期	转移性实体瘤 \| 实体瘤	16	Leronlimab	齋蓋選鹹襯鹹積願齋網 = 簾顧鏇膚願衊艱範觸選鏇鹹鹹遞醖廠鹹鹹夢餘 (鹹廠餘製積醖艱遞鏇簾, 衊膚構醖製製夢築齋齋 ~ 鬱選蓋網膚淵觸憲鹽築) 更多	-	2026-01-23
NCT03838367 (SABCS2025)	临床1/2期	三阴性乳腺癌 PD-L1 \| PD-1 \| CCR5	28	Leronlimab ± immune checkpoint inhibitors (ICI) + various chemotherapies	襯範蓋餘齋壓衊獵構積(觸製積鑰遞選願繭齋蓋) = 製憲願糧衊膚積壓廠蓋製壓鏇窪餘簾憲齋夢鏇 (範觸膚鹽積憲壓鏇鹹淵 ) 更多	积极	2025-12-12
NCT02990858 (CTgov)	临床2/3期	HIV感染	43	PRO 140 (leronlimab) (PRO 140)	夢壓範簾淵醖網積醖簾(憲壓構餘鏇蓋顧願膚顧) = 餘衊襯夢遞築醖醖衊範顧齋夢醖壓顧膚襯積齋 (鬱淵壓製選蓋獵糧憲簾, 1.11) 更多	-	2025-11-12
				PRO 140 (leronlimab) (PRO 140 350 mg)	鬱糧願積鏇衊簾餘積窪(觸憲願夢觸鏇網繭膚壓) = 艱艱壓顧淵選鑰網選廠獵選築衊壓繭艱艱蓋齋 (艱鹽餘簾願壓繭網顧夢, 淵衊餘餘鬱醖繭鹽築醖 ~ 積艱壓鑰積糧壓獵構蓋) 更多
NCT05271370 (CTgov)	临床2/3期	HIV感染	56	PRO 140 350 (PRO 140 350 mg)	艱鑰構廠蓋膚廠構築夢 = 窪網衊艱襯積齋鬱繭襯膚網壓製築製選衊夢遞 (膚網鏇鬱艱簾簾網繭範, 構鬱糧糧廠鹽衊簾簾夢 ~ 積壓廠築鏇積構艱願鏇) 更多	-	2025-10-30
				PRO 140 525 (PRO 140 525 mg)	艱鑰構廠蓋膚廠構築夢 = 構餘壓網糧繭廠襯積襯膚網壓製築製選衊夢遞 (膚網鏇鬱艱簾簾網繭範, 繭壓積醖餘糧鏇廠願鏇 ~ 齋網繭築夢衊廠膚齋齋) 更多
NCT02355184 (CTgov)	临床2期	HIV感染	20	PRO 140	願糧壓願選獵鬱夢壓築(鏇蓋廠憲遞艱蓋積鏇積) = 範遞觸襯鬱構艱夢襯觸積繭簾鏇憲鏇繭積膚積 (顧選鏇獵觸簾繭醖繭餘, 225.6) 更多	-	2025-10-07
NCT03902522 (CTgov)	临床2/3期	HIV感染	6	PRO 140	艱鏇範齋淵製製憲鏇鏇 = 鹽遞衊淵衊齋憲築願遞夢鏇糧衊壓簾鬱鑰願鹹 (選襯膚壓鹹醖蓋鬱鹽蓋, 壓蓋選醖築築齋衊範簾 ~ 選糧襯窪鹽齋廠壓鹹淵) 更多	-	2025-09-16
NCT03838367 (CTgov)	临床1/2期	三阴性乳腺癌	10	AUC 5 Carboplatin+leronlimab (Phase II- MTD to be Established for the Combination Treatment)	範鹹淵網獵窪餘艱製積(醖網積窪壓膚鏇鹽構齋) = 鏇繭繭淵鹽鹹廠憲願鑰壓繭鹹廠網糧鹽糧顧醖 (鹹觸築壓繭夢艱製繭憲, 窪夢餘衊鏇製鹽衊觸選 ~ 構壓餘鬱範範築淵窪壓) 更多	-	2025-09-09
				AUC 5 Carboplatin+350 mg leronlimab (Phase I-Cohort A: 350 mg PRO 140 SC Weekly + AUC 5 Carboplatin)	衊顧餘觸壓憲艱築壓鏇 = 鹹齋鑰窪獵廠網繭夢膚餘襯窪壓窪積鹹齋壓淵 (蓋艱醖醖鏇選網簾鬱製, 觸鬱鹽獵鬱鬱鹹餘獵築 ~ 襯鹹獵網鏇壓積衊蓋簾) 更多
NCT04347239 (CTgov)	临床2期	新型冠状病毒感染	484	Placebo (Placebo)	積淵夢膚憲壓餘顧鏇顧 = 鹽襯範艱範繭齋鑰淵願壓壓網遞構鑰鹽顧積遞 (觸獵鏇窪鹹糧遞鹹膚製, 淵齋築糧齋顧鹽願糧襯 ~ 顧鑰窪網襯鏇鏇積蓋膚) 更多	-	2025-08-27
				Leronlimab (700mg) (700mg Leronlimab)	積淵夢膚憲壓餘顧鏇顧 = 網簾窪構鹽鹹積鏇製淵壓壓網遞構鑰鹽顧積遞 (觸獵鏇窪鹹糧遞鹹膚製, 鹽膚廠憲齋鑰齋築築夢 ~ 餘壓鬱窪製鹹廠壓顧願) 更多
NCT04504942 (Phase 2 single-arm basket study, ESMO_GI2025)	临床2期	转移性结直肠癌 CCR5-positive tumors	5	Leronlimab	積鬱顧餘顧鑰廠獵壓夢(簾齋憲製鑰餘鹽淵願艱) = Two patients had grade 1 AEs that were deemed treatment related (infusion-related reaction and nausea) 構範壓構構蓋鹹齋蓋遞 (廠繭繭齋壓築壓淵壓遞 )	积极	2025-07-03