A Phase II Study Of Intravenous DX-8951f (EXATECAN MESYLATE) Administered Daily For Five Days Every Three Weeks To Pediatric Patients With Relapsed Or Refractory Rhabdomyosarcoma

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase II trial to study the effectiveness of exatecan mesylate in treating children who have relapsed or refractory rhabdomyosarcoma.

Start Date01 Jan 2003

Sponsor / Collaborator

Daiichi Sankyo Co., Ltd.

NCT00055952

/ CompletedPhase 2

A Phase II Study Of Intravenous DX-8951f (EXATECAN MESYLATE) Administered Daily For Five Days Every Three Weeks To Pediatric And Young Adult Patients With Ewing's Sarcoma (ES), Primitive Neuroectodermal Tumor (PNET), Or Desmoplastic Small Round Cell Tumor (DSRCT)

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase II trial to study the effectiveness of exatecan mesylate in treating patients who have relapsed or refractory Ewing's sarcoma or peripheral primitive neuroectodermal tumor or desmoplastic small round cell tumor.

Start Date01 Jan 2003

Sponsor / Collaborator

Daiichi Sankyo Co., Ltd.

NCT00045318

/ CompletedPhase 1IIT

A Phase I Study of DX-8951f (Exatecan Mesylate for Injection) in Patients With Renal Dysfunction

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase I trial to study the effectiveness of exatecan mesylate in treating patients who have advanced solid tumors and kidney dysfunction.

Start Date01 May 2002

Sponsor / Collaborator

Jonsson Comprehensive Cancer Center

[+1]

100 Clinical Results associated with Exatecan mesilate

100 Translational Medicine associated with Exatecan mesilate

100 Patents (Medical) associated with Exatecan mesilate

173

Literatures (Medical) associated with Exatecan mesilate

01 Oct 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

An intrinsically hydrophilic linker enables a stable, high-DAR exatecan-based HER2 ADC with potent antitumor activity

Article

Author: Feng, Chaoyang ; Ma, Jianglei ; Wu, Chenglong ; Huang, Jinkun ; Bao, Yiwen ; Heng, Xiaojie ; Zeng, Nan ; Yang, Tingting ; Ni, Dechun

Antibody-drug conjugates (ADCs) combine the targeting specificity of monoclonal antibodies with the potent cytotoxicity of small-molecule drugs. However, ADC development using Exatecan, a potent topoisomerase I inhibitor, has been challenged by its hydrophobicity, leading to aggregation, rapid clearance, and off-target toxicity. Herein, we report the design of an intrinsically hydrophilic drug-linker platform (SMP-70067-L) that enables the construction of a homogeneous Exatecan-based HER2-targeted ADC (SMP-70067-X) with a high drug-to-antibody ratio (DAR of 7.92). Similar to Trastuzumab deruxtecan (DS-8201a), which achieves high DAR without PEG or polysarcosine chains through a hydrophilic self-immolative spacer, SMP-70067-L integrates minimal hydrophilic elements, including a glutamic acid residue and a modified aromatic self-immolative spacer, to balance hydrophilicity, stability, and efficient payload release. The resulting ADC exhibits low aggregation (<1%), favorable plasma and thermal stability, and sustained exatecan release. SMP-70067-X demonstrates potent cytotoxicity in HER2-positive tumor cells (sub-nanomolar IC₅₀ values) and significantly enhanced antitumor efficacy compared to DS-8201a in HER2-moderate and HER2-low xenograft models. These results highlight the critical role of rational linker engineering in expanding the therapeutic window of hydrophobic topoisomerase I inhibitor-based ADCs.

02 Jul 2026·MOLECULAR CANCER THERAPEUTICS

Identification and Preclinical Evaluation of a Novel GD2 Antibody–Drug Conjugate for Solid Tumors in Children and Adults

Article

Author: Li, Jing ; Song, Deyong ; Teng, Yanni ; Dou, Changlin ; Rao, Muding ; Wang, Qiaoping ; Zhu, Xiaolin ; Dong, Chuangchuang ; Han, Jing ; Xiao, Min ; Liu, Hong ; Ma, Zhuqing

Abstract:

The ganglioside GD2 is an attractive cancer target because of its high expression in neuroblastoma and other solid tumors with limited normal-tissue distribution. Despite regulatory approvals of three anti-GD2 antibodies, clinical efficacy remains limited by neurotoxicity, suboptimal affinity for antibody-dependent cellular cytotoxicity (ADCC), and immunogenicity. Developing a highly effective, less toxic anti-GD2 agent remains an unmet need. In this study, a novel anti-GD2 murine antibody, CA450, was identified by immunizing mice with GD2 conjugated to keyhole limpet hemocyanin or Qβ virus–like particles, followed by phage display screening. The humanized version, hCA450-21, displayed higher cell-binding activity than ch14.18 and Hu3F8, along with excellent specificity and internalization capacity. To overcome the limitations of traditional anti-GD2 antibody therapy, hCA450-21 was engineered and conjugated to exatecan to create an antibody–drug conjugate (ADC), which may reduce or avoid neurotoxicity by employing a mechanism distinct from ADCC and complement-dependent cytotoxicity. The hCA450-21.1-LA-68B ADC demonstrated potent in vitro cytotoxicity against glioblastoma, melanoma, and breast cancer cell lines and in vivo tumor growth inhibition in LN229 and SK-MEL-5 xenograft models. Toxicity studies in mice showed a favorable safety profile, with reduced neurotoxicity compared with naked antibody therapy by ch14.18-IgG1 and hCA450-21.1-IgG1. The crystal structure of the hCA450-21.1 Fab–GD2 complex was resolved at 1.69 Å, revealing unique hydrogen bonds and hydrophobic interactions that contribute to its high specificity and affinity. Overall, the novel hCA450-21.1-LA-68B ADC shows preclinical efficacy and reduced toxicity, particularly neurotoxicity, indicating potential as a safer and more effective therapy for GD2-positive pediatric and adult tumors.

01 Jun 2026·DRUGS

Sequential Use of Trastuzumab Deruxtecan and Sacituzumab Govitecan in Patients with Breast Cancer: A Pharmacological Approach to Support the Clinical Rationale

Review

Author: Mathijssen, Ron H J ; Bria, Emilio ; Curigliano, Giuseppe ; Danesi, Romano ; Inglese, Elvira ; Del Re, Marzia ; Blok, Erik J

Antibody-drug conjugates (ADCs) represent a major advance in breast cancer therapy, with trastuzumab deruxtecan and sacituzumab govitecan emerging as leading agents targeting distinct tumor antigens and employing different linker-payload designs. Trastuzumab deruxtecan is a second-generation HER2-directed ADC composed of trastuzumab linked via a cleavable tetrapeptide linker to the camptothecin derivative exatecan, a highly potent topoisomerase I inhibitor. Its high drug-to-antibody ratio (DAR 8:1), membrane-permeable payload, and efficient lysosomal release confer strong antitumor activity, including a robust bystander effect in HER2-low tumors. By contrast, sacituzumab govitecan is a TROP-2-targeted ADC conjugated through a hydrolysable CL2A linker to SN-38, the active metabolite of irinotecan. Sacituzumab govitecan features a high DAR (7.6:1) and allows extracellular as well as intracellular release of SN-38, enhancing bystander killing in tumors with heterogeneous TROP-2 expression, while maintaining a favorable toxicity profile due to the lower intrinsic potency of SN-38 relative to exatecan. Since both these ADCs are conjugated to topoisomerase I inhibitors, concerns about potential cross-resistance regarding their sequencing in clinical practice are being raised, and currently there is a lack of predictive biomarkers providing a rational basis for their sequential administration. Resistance mechanisms exhibit significant heterogeneity: resistance to trastuzumab deruxtecan has been associated with mutations in TOPO I and SLX4, impaired lysosomal function, and efflux via ABC transporters. In contrast, resistance to sacituzumab govitecan is linked to overexpression of multidrug resistance proteins, particularly BCRP-mediated efflux. Clinically, trastuzumab deruxtecan has shown substantial efficacy in both HER2-positive and HER2-low breast cancer, whereas sacituzumab govitecan has demonstrated efficacy across triple-negative and hormone receptor-positive/HER2-negative breast cancers. Collectively, these agents highlight how variations in target antigen, linker chemistry, and payload potency impact ADC activity, therapeutic index, and potential strategies for sequential treatment in advanced breast cancer.

395

News (Medical) associated with Exatecan mesilate

31 Jul 2026

·www.biospace.com

Datroway® Approved in the EU as Only TROP2 Directed Medicine with Overall Survival Benefit for the First-Line Treatment of Patients with Metastatic TNBC Who Are Not Candidates for Immunotherapy

Approval based on TROPION-Breast02 phase 3 trial results where Daiichi Sankyo and AstraZeneca’s Datroway showed a statistically significant and clinically meaningful improvement for the dual primary endpoints of overall survival and progression-free survival Datroway now approved for two breast cancer indications in the EU TOKYO--(BUSINESS WIRE)--Datroway ® (datopotamab deruxtecan) has been approved in the European Union (EU) as monotherapy for the first-line treatment of adult patients with unresectable or metastatic triple negative breast cancer (TNBC) who are not candidates for PD-1/PD-L1 inhibitor therapy. Datroway is a specifically engineered TROP2 directed DXd antibody drug conjugate (ADC) discovered by Daiichi Sankyo (TSE: 4568) and being jointly developed and commercialized by Daiichi Sankyo and AstraZeneca (LSE/STO/NYSE: AZN). The approval by the European Commission follows the positive opinion of the Committee for Medicinal Products for Human Use of the European Medicines Agency and is based on results from the TROPION-Breast02 phase 3 trial, which were presented at the 2025 European Society for Medical Oncology Congress and subsequently published in Annals of Oncology . In TROPION-Breast02, which included patients with metastatic TNBC who experienced early relapse following prior treatment, Datroway demonstrated a statistically significant and clinically meaningful 5.0 month improvement in median overall survival (OS) versus investigator’s choice of chemotherapy (hazard ratio [HR]=0.79; 95% confidence interval [CI]: 0.64-0.98; p=0.0291). Median OS was 23.7 months for patients treated with Datroway versus 18.7 months for those treated with chemotherapy. Datroway reduced the risk of disease progression or death by 43% compared to chemotherapy (HR=0.57; 95% CI: 0.47-0.69; p<0.0001) as assessed by blinded independent central review (BICR). Median progression-free survival (PFS) was 10.8 months for patients treated with Datroway versus 5.6 months for those treated with chemotherapy in patients with metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy. Datroway also was associated with more robust treatment responses compared to chemotherapy, with an objective response rate (ORR) of 62.5% versus 29.3% for those treated with chemotherapy. ezstandalone.cmd.push(function () { ezstandalone.showAds(131); }); “For people living with metastatic triple negative breast cancer, every new treatment option matters. Despite recent advances, more than two thirds of patients are not candidates for immunotherapy and have had limited options beyond chemotherapy,” said Giuseppe Curigliano, MD, PhD, Director of the Early Drug Development Division, European Institute of Oncology, Professor of Medical Oncology, University of Milan, Italy and investigator for the TROPION-Breast02 trial. “In my practice, I see firsthand the devastating impact this aggressive disease has on patients and their families. This approval of datopotamab deruxtecan provides a new treatment option for eligible patients and represents meaningful progress.” The safety pro Datroway (6 mg/kg) was evaluated in 319 patients with TNBC who received Datroway in TROPION-Breast02. The most common (≥20%) adverse reactions, including laboratory abnormalities, were stomatitis, increased amylase, nausea, alopecia, decreased hemoglobin, decreased white blood cells, constipation, decreased calcium, decreased lymphocytes, fatigue, decreased neutrophils, increased alanine aminotransferase, increased aspartate aminotransferase, dry eye, keratitis, decreased albumin, vomiting, musculoskeletal pain, decreased sodium and increased blood alkaline phosphatase. Serious adverse reactions occurred in 17% of patients who received Datroway. Serious adverse reactions in more than 1% of patients who received Datroway included pneumonia, vomiting, COVID-19 and anemia. One patient fatality was attributed to interstitial lung disease/pneumonitis. “With this approval, Datroway is the only TROP2 directed antibody drug conjugate approved in the EU that has demonstrated an overall survival benefit in the first-line setting, representing a meaningful advance for the treatment of patients with metastatic triple negative breast cancer,” said Ken Keller, Global Head of Oncology Business, and President and CEO, Daiichi Sankyo, Inc. “We look forward to bringing Datroway to patients in the EU as an additional treatment option with the potential to extend survival, reflecting our commitment to advancing innovative medicines that address unmet needs for people living with cancer.” “Every year, more than 80,000 people in Europe are diagnosed with triple negative breast cancer, a disease that often affects younger women and has limited treatment options in the metastatic setting,” said Dave Fredrickson, Executive Vice President, Oncology Hematology Business Unit, AstraZeneca. “Today’s approval of Datroway brings an antibody drug conjugate with a differentiated clinical pro by a strong survival benefit to people with this aggressive disease.” Based on the results of TROPION-Breast02, Datroway has been included in the ESMO Clinical Practice Guidelines as a Category IA first-line treatment option for patients with metastatic TNBC who are not candidates for immunotherapy, and it is the preferred option for patients who have relapsed within six months of completing adjuvant therapy. 1 Datroway also received a score of four out of five on the ESMO Magnitude of Clinical Benefit Scale (ESMO-MCBS), recognizing the clinically meaningful benefit demonstrated in TROPION-Breast02. 2 Datroway (6 mg/kg) was approved in the U.S. in May 2026 for the treatment of adult patients with unresectable or metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy. Additional reviews are underway in China and Japan, as well as Australia, Canada, Singapore and Switzerland as part of Project Orbis. About TROPION-Breast02 TROPION-Breast02 is a global, multicenter, randomized, open-label phase 3 trial evaluating the efficacy and safety of Datroway versus investigator’s choice of chemotherapy (paclitaxel, nab-paclitaxel, capecitabine, carboplatin or eribulin) in patients with previously untreated locally recurrent inoperable or metastatic TNBC for whom immunotherapy was not an option. This included patients whose tumors did not express PD-L1 as well as patients with PD-L1 expressing tumors who could not receive immunotherapy due to prior exposure in early-stage disease, comorbidities or immunotherapy not being accessible in their geography. Enrollment included patients with de novo or recurrent disease, regardless of disease-free interval, and those with poor prognostic factors such as stable brain metastases. The dual primary endpoints of TROPION-Breast02 are OS and PFS as assessed by BICR. Secondary endpoints include PFS as assessed by investigator, ORR, duration of response, disease control rate, pharmacokinetics and safety. TROPION-Breast02 enrolled 644 patients at sites in Africa, Asia, Europe, North America and South America. For more information visit ClinicalTrials.gov . About Triple Negative Breast Cancer TNBC accounts for approximately 15% of all breast cancer cases, with an estimated 365,000 diagnoses globally each year. 3,4 In Europe, there are an estimated 81,000 diagnoses of TNBC each year. 3,5 TNBC is diagnosed more frequently in younger and premenopausal women, and is more prevalent in Black and Hispanic women. 6,7,8 Metastatic TNBC is the most aggressive type of breast cancer and has one of the worst prognoses, with median OS of just 12 to 18 months and only about 15% of patients living five years following diagnosis. 6,9,10 While some breast cancers may test positive for estrogen receptors, progesterone receptors or overexpression of HER2, TNBC tests negative for all three. 6 Due to its aggressive nature and absence of common breast cancer receptors, TNBC is characteristically difficult to treat. 6 For patients with metastatic disease with PD-L1 expressing tumors, the addition of immunotherapy to chemotherapy has improved outcomes in the first-line setting. 11,12 However, for approximately 70% of patients with metastatic TNBC who are not candidates for immunotherapy, chemotherapy was the standard first-line treatment. 13 TROP2 is a protein broadly expressed in several solid tumors, including TNBC. 14 TROP2 is associated with increased tumor progression and poor survival in patients with breast cancer. 15,16 About Datroway Datroway (datopotamab deruxtecan; datopotamab deruxtecan-dlnk in the U.S. only) is a TROP2 directed ADC. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology, Datroway is one of seven DXd ADCs in the oncology pipeline of Daiichi Sankyo, and one of the most advanced programs in AstraZeneca’s ADC scientific platform. Datroway is comprised of a humanized anti-TROP2 IgG1 monoclonal antibody, developed in collaboration with Sapporo Medical University, attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. Datroway (6 mg/kg) is approved in more than 30 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy based on the results from the TROPION-Breast02 trial. Datroway (6 mg/kg) is approved in more than 45 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HR positive, HER2 negative (IHC 0, IHC 1+ or IHC 2+/ISH-) breast cancer who have received prior endocrine-based therapy and chemotherapy for unresectable or metastatic disease based on the results from the TROPION-Breast01 trial. Datroway (6 mg/kg) is approved in Brazil, Russia, Singapore and the U.S. for the treatment of adult patients with locally advanced or metastatic EGFR-mutated non-small cell lung cancer (NSCLC) who have received prior EGFR-directed therapy and platinum-based chemotherapy, based on the results from TROPION-Lung05 and TROPION-Lung01 trials. Continued approval for this indication in the U.S. may be contingent upon verification and description of clinical benefit in a confirmatory trial. About the Datroway Clinical Development Program A comprehensive global clinical development program is underway with more than 20 trials evaluating the efficacy and safety of Datroway across multiple cancers, including NSCLC, TNBC and urothelial cancer. The program includes eight phase 3 trials in lung cancer, five phase 3 trials in breast cancer, and one phase 2/3 trial in urothelial cancer evaluating Datroway as a monotherapy and in combination with other cancer treatments in various settings. About the Daiichi Sankyo and AstraZeneca Collaboration Daiichi Sankyo and AstraZeneca entered into a global collaboration to jointly develop and commercialize Enhertu ® in March 2019 and Datroway in July 2020 , except in Japan where Daiichi Sankyo maintains exclusive rights for each ADC. Daiichi Sankyo is responsible for the manufacturing and supply of Enhertu and Datroway. About the ADC Portfolio of Daiichi Sankyo The Daiichi Sankyo ADC portfolio consists of eight ADCs in clinical development crafted from ADC technology discovered in-house by Daiichi Sankyo. The DXd ADC Technology platform of Daiichi Sankyo consists of seven ADCs in clinical development where each ADC is comprised of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. The DXd ADCs include Enhertu and Datroway, which are being jointly developed and commercialized globally with AstraZeneca, and ifinatamab deruxtecan (I-DXd), raludotatug deruxtecan (R-DXd) and patritumab deruxtecan (HER3-DXd), which are being jointly developed and commercialized globally with Merck & Co., Inc, Rahway, NJ, USA. DS-3939 and DS3790 are being developed by Daiichi Sankyo. An additional ADC being developed by Daiichi Sankyo is DS3610, which consists of an antibody attached to a novel payload that acts as an agonist of STING. Ifinatamab deruxtecan, raludotatug deruxtecan, patritumab deruxtecan, DS-3939, DS3610 and DS3790 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established. About Daiichi Sankyo Daiichi Sankyo (TSE: 4568) is a global healthcare company committed to becoming a trusted healthcare innovator, transforming the lives of people through its strength in science and technology. The company discovers and develops new standards of care to address diverse medical needs to fulfill its purpose of contributing to the enrichment of quality of life around the world. With a strategic focus on oncology, Daiichi Sankyo is advancing an industry-leading antibody drug conjugate portfolio along with identifying new breakthrough generating technologies to deliver practice-changing medicines to patients, healthcare professionals and society. For more information, please visit . ____________________ REFERENCES: 1 de Azambuja E, et al., Annals of Oncology . 2026 2 ESMO. ESMO-MCBS Scorecard: Datopotamab deruxtecan . Accessed July 2026 3 O’Reilly D, et al. World J Clin Oncol . 2021;12(3):164-182. 4 World Health Organization. Global Status Report on Cancer 2026 . Accessed July 2026. 5 World Health Organization. Global Cancer Observatory: Europe . Accessed July 2026. 6 American Cancer Society. Triple-Negative Breast Cancer . Accessed July 2026. 7 Martinez M, et al. Breast Cancer Res Treat . 2017;166(1):185-193. 8 Vargas L, et al. Cancer Epidemiol Biomarkers Prev . 2019;28(11):1771-1783. 9 National Cancer Institute . SEER Cancer Stat Facts: Female Breast Cancer Subtypes . Accessed July 2026. 10 Huppert L, et al. Ther Adv Med Oncol . 2022;14:1-25. 11 Cortes J, et al. N Engl J Med . 2022;387:217-226. 12 Geurts V, et al. Curr Treat Options Oncol . 2023;24:628-643. 13 Punie K, et al. Oncologist . 2025;30(3):oyaf034. 14 Rossi V, et al. Front Immunol . 2024;15:1447280. 15 Lin H, et al. Exp Mol Pathol . 2013:94(1):73-78. 16 Goldenberg D, et al. Oncotarget . 2018;9(48):28989-29006. Contacts MEDIA CONTACTS: Global: Jennifer Brennan jennifer.brennan@daiichisankyo.com +1 908 900 3183 (mobile) EU: Simone Jendsch-Dowé simone.jendsch-dowe@daiichisankyo.com +49 (89) 78080 (office) Japan: DS-PR_jp@daiichisankyo.com INVESTOR RELATIONS CONTACT: DaiichiSankyoIR_jp@daiichisankyo.com

30 Jul 2026

·www.biospace.com

Promatix Biosciences Awarded Innovate UK Biomedical Catalyst Grant to Advance First-in-Class EGFR × EphA2 Cis-Bispecific ADC

Promatix Biosciences Awarded Innovate UK Biomedical Catalyst Grant to Advance First-in-Class EGFR × EphA2 Cis-Bispecific ADC Non-dilutive Biomedical Catalyst funding from Innovate UK will support the advancement of Promatix's lead cis-bispecific antibody-drug conjugate (ADC), PBS293-exatecan, towards development candidate nomination Award funds manufacturing scale-up, additional preclinical proof-of-concept in cell-line-derived (CDX) and patient-derived (PDX) xenograft models, and IND-enabling regulatory safety studies Programme also expands the potential of Promatix’s lead EGFR x EphA2 programme beyond colorectal cancer (CRC), with the same tumour-selective approach now being applied to oesophageal cancer and non-small cell lung cancer (NSCLC) London and Cambridge, UK, July 28, 2026 (GLOBE NEWSWIRE) -- Promatix Biosciences Ltd (Promatix), an emerging UK-based biotechnology company developing innovative new classes of cancer therapies using cis-bispecific antibodies, today announced that it has been awarded a grant under the Innovate UK Biomedical Catalyst 2025: Industry-led R&D small projects competition. The funding will support continued development of the Company's lead programme, PBS293-exatecan, a first-in-class EGFR × EphA2 cis-bispecific ADC for the treatment of CRC and other solid tumours. The award will fund the scale-up and conjugation of PBS293 with an exatecan payload, additional preclinical proof-of-concept studies in both CDX and PDX models of CRC, and IND-enabling regulatory safety studies to support the nomination of PBS293-exatecan as a development candidate. In parallel, Promatix will apply its discovery platform to evaluate oesophageal cancer and NSCLC as additional indications. The work will be conducted with established UK-based contract research organisations, including Abzena, Crown Bioscience and Labcorp UK. PBS293 targets EGFR and EphA2, two antigens co-expressed on colorectal tumour cells. While EGFR is a clinically validated target in CRC, the benefit of EGFR-targeted antibodies such as cetuximab is limited to a subset of patients and constrained by toxicity arising from EGFR expression in healthy tissue. Building on previously reported preclinical data, Promatix has advanced an exatecan-based conjugate, selected for its established clinical safety pro efficacy. In preclinical studies, PBS293-exatecan has demonstrated potent killing of colorectal cancer cell lines while substantially sparing normal human keratinocytes and endothelial cells — consistent with the tumour-selective “AND-gate” design intended to widen the therapeutic window. ezstandalone.cmd.push(function () { ezstandalone.showAds(131); }); “This award from Innovate UK enables us to generate the additional preclinical data needed to move PBS293-exatecan towards development candidate nomination,” said Dr. Roy Pettipher, Chief Scientific Officer and Co-Founder of Promatix . “By scaling up our lead conjugate and testing it in both cell-line and patient-derived models, alongside the regulatory safety studies expected for an ADC, we plan to assemble the industry-standard data package that partners and investors are looking for. PBS293-exatecan combines potent tumour-cell killing with sparing of normal skin and vascular cells in our preclinical work, reflecting the tumour selectivity that is central to our cis-bispecific approach.” “Non-dilutive funding of this kind is strong external validation of both our lead programme and the proteomics-driven discovery platform behind it,” said Dr. Michael Hunter, CEO and Co-Founder of Promatix . “It will enable us to advance PBS293-exatecan in colorectal cancer while extending the same logic-gated approach to further solid tumours, including oesophageal and non-small cell lung cancer. Generating robust efficacy and safety data in this programme is a key inflection point that we expect to underpin a future pharma partnership and to support our planned Series A financing, enabling us to build a broader pipeline of tumour-selective bispecific ADCs from a UK base.” The programme reinforces Promatix's integrated platform, which combines large-scale tumour surface proteomics with logic-gated computational modelling to identify complementary antigen pairs and expand the universe of tumour-selective targets available for next-generation ADCs. EGFR × EphA2 was identified and prioritised through this platform, and success in the funded programme is intended to provide further validation of the approach across additional cancer indications. About PBS293-exatecan PBS293-exatecan is a full IgG1 cis-bispecific antibody-drug conjugate targeting EGFR and EphA2, in development for advanced colorectal cancer. Through cis-bispecific “AND-gate” targeting, strong binding, payload delivery and uptake occur only when both antigens are present on the same tumour cell. PBS293 is designed to address a broader patient population than current EGFR-targeted antibodies — independent of RAS/BRAF mutation status and including right-sided colorectal tumours, for which treatments such as cetuximab are ineffective. About the Innovate UK Biomedical Catalyst The Biomedical Catalyst is an Innovate UK programme supporting innovative UK businesses to develop solutions to health and healthcare challenges. Innovate UK, part of UK Research and Innovation, is creating a better future by inspiring, involving and investing in businesses developing life-changing innovations. Innovate UK provides targeted sectors with expertise, facilities and funding to test, demonstrate and evolve their ideas, driving UK productivity and economic growth. About Promatix Biosciences Ltd Promatix is a UK-based oncology drug discovery and development company developing next-generation bispecific antibody-drug conjugates (ADCs) through rational, data-driven cis-target pairing. The Company's approach centres on identifying optimal combinations of cancer surface markers for cis-bispecific “AND-gate” targeting, in which strong binding, payload delivery and uptake occur only when two distinct antigens are present on the same tumour cell. This dual-antigen engagement is designed to enhance tumour selectivity. By exploiting hybrid avidity, Promatix aims to reduce on-target off-tumour toxicity, enhance efficacy and expand the range of targets that can be addressed with ADCs. At the core of the platform is TxPro, a comprehensive tumour surface proteomics database covering membrane proteins across multiple cancer types. TxPro is supported by proprietary computational analytics (CipherPro) to systematically mine tumour-selective antigen pairs, affinity-engineering capabilities (AviPro) to optimise bispecific engagement, and a modular functional validation framework for rapid evaluation and lead selection (BiPro). Promatix is developing a pipeline of novel bispecific ADCs in colorectal cancer and additional solid tumour indications. For more information, visit and follow us on LinkedIn. CONTACT: CONTACT INFORMATION: Promatix Biosciences Ltd info@promatix.com MEDIA CONTACT: MC Services AG Julia Bittner +49 211 529 252 28 In the US: Laurie Doyle +1 339 832 0752 promatix@mc-services.eu

ADC

29 Jul 2026

·www.biospace.com

Promatix Biosciences Innovate UK Biomedical Catalyst Grant

Promatix Biosciences Awarded Innovate UK Biomedical Catalyst Grant to Advance First-in-Class EGFR × EphA2 Cis-Bispecific ADC • Non-dilutive Biomedical Catalyst funding from Innovate UK will support the advancement of Promatix's lead cis-bispecific antibody-drug conjugate (ADC), PBS293-exatecan, towards development candidate nomination • Award funds manufacturing scale-up, additional preclinical proof-of-concept in cell-line-derived (CDX) and patient-derived (PDX) xenograft models, and IND-enabling regulatory safety studies • Programme also expands the potential of Promatix’s lead EGFR x EphA2 programme beyond colorectal cancer (CRC), with the same tumour-selective approach now being applied to oesophageal cancer and non-small cell lung cancer (NSCLC) London and Cambridge, UK, July 28 2026 (GLOBE NEWSWIRE) -- Promatix Biosciences Ltd (Promatix), an emerging UK-based biotechnology company developing innovative new classes of cancer therapies using cis-bispecific antibodies, today announced that it has been awarded a grant under the Innovate UK Biomedical Catalyst 2025: Industry-led R&D small projects competition. The funding will support continued development of the Company's lead programme, PBS293-exatecan, a first-in-class EGFR × EphA2 cis-bispecific ADC for the treatment of CRC and other solid tumours. The award will fund the scale-up and conjugation of PBS293 with an exatecan payload, additional preclinical proof-of-concept studies in both CDX and PDX models of CRC, and IND-enabling regulatory safety studies to support the nomination of PBS293-exatecan as a development candidate. In parallel, Promatix will apply its discovery platform to evaluate oesophageal cancer and NSCLC as additional indications. The work will be conducted with established UK-based contract research organisations, including Abzena, Crown Bioscience and Labcorp UK. PBS293 targets EGFR and EphA2, two antigens co-expressed on colorectal tumour cells. While EGFR is a clinically validated target in CRC, the benefit of EGFR-targeted antibodies such as cetuximab is limited to a subset of patients and constrained by toxicity arising from EGFR expression in healthy tissue. Building on previously reported preclinical data, Promatix has advanced an exatecan-based conjugate, selected for its established clinical safety profile and efficacy. In preclinical studies, PBS293-exatecan has demonstrated potent killing of colorectal cancer cell lines while substantially sparing normal human keratinocytes and endothelial cells — consistent with the tumour-selective “AND-gate” design intended to widen the therapeutic window. “This award from Innovate UK enables us to generate the additional preclinical data needed to move PBS293-exatecan towards development candidate nomination,” said Dr. Roy Pettipher, Chief Scientific Officer and Co-Founder of Promatix . “By scaling up our lead conjugate and testing it in both cell-line and patient-derived models, alongside the regulatory safety studies expected for an ADC, we plan to assemble the industry-standard data package that partners and investors are looking for. PBS293-exatecan combines potent tumour-cell killing with sparing of normal skin and vascular cells in our preclinical work, reflecting the tumour selectivity that is central to our cis-bispecific approach.” “Non-dilutive funding of this kind is strong external validation of both our lead programme and the proteomics-driven discovery platform behind it,” said Dr. Michael Hunter, CEO and Co-Founder of Promatix . “It will enable us to advance PBS293-exatecan in colorectal cancer while extending the same logic-gated approach to further solid tumours, including oesophageal and non-small cell lung cancer. Generating robust efficacy and safety data in this programme is a key inflection point that we expect to underpin a future pharma partnership and to support our planned Series A financing, enabling us to build a broader pipeline of tumour-selective bispecific ADCs from a UK base.” The programme reinforces Promatix's integrated platform, which combines large-scale tumour surface proteomics with logic-gated computational modelling to identify complementary antigen pairs and expand the universe of tumour-selective targets available for next-generation ADCs. EGFR × EphA2 was identified and prioritised through this platform, and success in the funded programme is intended to provide further validation of the approach across additional cancer indications. About PBS293-exatecan PBS293-exatecan is a full IgG1 cis-bispecific antibody-drug conjugate targeting EGFR and EphA2, in development for advanced colorectal cancer. Through cis-bispecific “AND-gate” targeting, strong binding, payload delivery and uptake occur only when both antigens are present on the same tumour cell. PBS293 is designed to address a broader patient population than current EGFR-targeted antibodies — independent of RAS/BRAF mutation status and including right-sided colorectal tumours, for which treatments such as cetuximab are ineffective. About the Innovate UK Biomedical Catalyst The Biomedical Catalyst is an Innovate UK programme supporting innovative UK businesses to develop solutions to health and healthcare challenges. Innovate UK, part of UK Research and Innovation, is creating a better future by inspiring, involving and investing in businesses developing life-changing innovations. Innovate UK provides targeted sectors with expertise, facilities and funding to test, demonstrate and evolve their ideas, driving UK productivity and economic growth. About Promatix Biosciences Ltd Promatix is a UK-based oncology drug discovery and development company developing next-generation bispecific antibody-drug conjugates (ADCs) through rational, data-driven cis-target pairing. The Company's approach centres on identifying optimal combinations of cancer surface markers for cis-bispecific “AND-gate” targeting, in which strong binding, payload delivery and uptake occur only when two distinct antigens are present on the same tumour cell. This dual-antigen engagement is designed to enhance tumour selectivity. By exploiting hybrid avidity, Promatix aims to reduce on-target off-tumour toxicity, enhance efficacy and expand the range of targets that can be addressed with ADCs. At the core of the platform is TxPro, a comprehensive tumour surface proteomics database covering membrane proteins across multiple cancer types. TxPro is supported by proprietary computational analytics (CipherPro) to systematically mine tumour-selective antigen pairs, affinity-engineering capabilities (AviPro) to optimise bispecific engagement, and a modular functional validation framework for rapid evaluation and lead selection (BiPro). Promatix is developing a pipeline of novel bispecific ADCs in colorectal cancer and additional solid tumour indications. For more information, visit and follow us on LinkedIn. CONTACT INFORMATION: Promatix Biosciences Ltd info@promatix.com MEDIA CONTACT: MC Services AG Julia Bittner +49 211 529 252 28 In the US: Laurie Doyle +1 339 832 0752 promatix@mc-services.eu

100 Deals associated with Exatecan mesilate

External Link

KEGG	Wiki	ATC	Drug Bank
D01432	Exatecan mesilate	-	DB12185

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pancreatic Cancer	Phase 3	United States	Daiichi Sankyo Co., Ltd.	01 Jul 2001
Pancreatic Cancer	Phase 3	Canada	Daiichi Sankyo Co., Ltd.	01 Jul 2001
Desmoplastic Small Round Cell Tumor	Phase 2	United States	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Desmoplastic Small Round Cell Tumor	Phase 2	Canada	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Peripheral Primitive Neuroectodermal Tumors	Phase 2	United States	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Peripheral Primitive Neuroectodermal Tumors	Phase 2	Canada	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Recurrent Ewing Sarcoma	Phase 2	United States	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Recurrent Ewing Sarcoma	Phase 2	Canada	Daiichi Sankyo Co., Ltd.	01 Jan 2003
Esophageal Carcinoma	Phase 2	United States	Daiichi Sankyo Co., Ltd.	01 Apr 2001
Esophageal Carcinoma	Phase 2	Canada	Daiichi Sankyo Co., Ltd.	01 Apr 2001

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed \| Eur J Cancer	Phase 2	Locally Advanced Soft Tissue Sarcoma	-	Exatecan	nkxklfewyx(tyjpnoxffp) = qbhnhahybf ohyszycgqy (embphhqphj ) View more	Negative	01 Apr 2007
Pubmed \| J Clin Oncol	Phase 3	Advanced Pancreatic Adenocarcinoma First line	349	Exatecan plus gemcitabine	ycepxgucmn(nmjvyopulh) = jtiojgbiia ffvzimlgwa (jvrxavyqxe ) View more	Negative	20 Sep 2006
Pubmed \| J Clin Oncol	Phase 3	Advanced Pancreatic Adenocarcinoma First line	349	Gemcitabine alone	ycepxgucmn(nmjvyopulh) = jgzzdvdoqn ffvzimlgwa (jvrxavyqxe ) View more	Negative	20 Sep 2006
ASCO2004	Phase 2	Metastatic Gastric Carcinoma	41	DX-8951f	xcwnsiygpa(zrvasjyxmd) = qsjgdeovrx uecwegkykp (jkitbthvce )	-	15 Jul 2004
ASCO2004	Phase 3	Pancreatic Cancer	349	DX-8951f (Exatecan Mesylate; DX) + Gemcitabine (GEM)	mrnaqlvuhm(vqbtgfavdh) = gprptqrupc oddrxxokcl (dzgeovqrvp ) View more	Negative	15 Jul 2004
ASCO2004	Phase 3	Pancreatic Cancer	349	Gemcitabine (GEM)	mrnaqlvuhm(vqbtgfavdh) = qoiatrnurz oddrxxokcl (dzgeovqrvp ) View more	Negative	15 Jul 2004
ASCO2004	Phase 3	Pancreatic Cancer	339	Ensiv	defpochomo(vwsgblvjcw) = xzsnvspzgw vkjndksmmp (ibqjesgtdc ) View more	-	15 Jul 2004
ASCO2004	Phase 3	Pancreatic Cancer	339	Gemcitabine	defpochomo(vwsgblvjcw) = xixcomsspy vkjndksmmp (ibqjesgtdc ) View more	-	15 Jul 2004
Pubmed \| Lung Cancer	Phase 2	Advanced Lung Non-Small Cell Carcinoma First line	39	Exatecan mesylate (DX-8951f)	bwbhbcovpd(ugwyijajzx) = edyuelyrtm iihktzhyus (qdsmvobsrg ) View more	Negative	01 Aug 2003

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