Cited by 280interferon and immune responsesCancer Immunotherapy and BiomarkersImmunotherapy and Immune Responses

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Preliminary results of the first-in-human (FIH) study of MK-1454, an agonist of stimulator of interferon genes (STING), as monotherapy or in combination with pembrolizumab (pembro) in patients with advanced solid tumors or lymphomas

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Harrington, K.J., Brody, J., Ingham, M., Strauss, J., Cemerski, S., Wang, M., Tse, A., Khilnani, A., Marabelle, A., Golan, T.·2018·Annals of Oncology

DOI 10.1093/annonc/mdy424.015

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“The most common adverse events were pyrexia, fatigue, nausea, and pruritus [212].”
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Targeting STING to generate therapeutic anti-tumor immunity
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STING activation disrupts tumor vasculature to overcome the EPR limitation and increase drug deposition
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“Systemic delivery of CDN-based STING agonists is limited by their poor PK and instability in plasma ( 34 , 58 – 60 ).”
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“Lung cancer patients with this tumor genetic profile showed a worse response to ICI than did patients with KRASmutant tumors without LKB1 co-mutations (27–30).”
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RIG-I-induced innate antiviral immunity protects mice from lethal SARS-CoV-2 infection
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“77,125 129 However, the underwhelming results of this approach underline the challenge of applying STING agonists in the clinic.”
Background
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Gangar, M., Goyal, S., Raykar, D., Khurana, P., Martis, A. M., Goswami, A., Ghoshal, I., Patel, K. V., Nagare, Y. K., Raikar, S. S., et al. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105549 · Cited by 31
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“MK-1454, a synthetic CDN which binds directly to STING, showed a safe tolerability profile and encouraging efficacy together with pembrolizumab in a phase I trial (NCT03010176) (Harrington et al., 2018).”
Background
Pharmacologic Activation of STING in the Bladder Induces Potent Antitumor Immunity in Non–Muscle Invasive Murine Bladder Cancer
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“Despite this agonist being suggested to harbor a boosting effect when co-administered with humanized anti-PD-1 antibody, adverse side effects were still observed, indicating a lack of efficiency [70,73,74].”
Phase 1 first-in-human dose-escalation study of IMSA101, a novel cyclic di-nucleotide STING agonist, for patients with advanced solid tumor malignancies
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“36 In our study, FLOT1 depletion enhanced the activation of STING pathway by boosting DNA damage and increasing the accumulation of dsDNA in cytoplasm after delivery of radiation, which might compensate for the limitation of the exogenous CDN delivery – low cell permeability and unsatisfied…”
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“Although several STING agonists are undergoing pre-clinical and clinical trials, the major drawbacks of available STING agonists include poor pharmacokinetic and physicochemical properties, as well as risks of cytokine release syndrome in the case of systemic administration, thereby largely restricting them to intra-t…”
Background
Bioactive metallic nanoparticles for synergistic cancer immunotherapy
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“There are also non-nucleotide STING agonists ( e.g. , MSA-2 226 , MK-1454 227 , and ADU-S100 228 ) and nucleotide-based STING agonists ( e.g. , interferon-stimulated DNA (ISD) 58 , 2 0 -3 0 -cyclic GMP e AMP 229 , cyclic-di-GMP 230 , exo-STING).”
Conjugated STING agonists
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“Another synthetic STING agonist, MK-1454, demonstrates potent antitumour activity in pre-clinical trials and is currently in clinical development, showing encouraging efficacy (Harrington et al., 2018; Chang W. et al., 2022).”
Background
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“STING agonists as anticancer agents have robust preclinical evidence; phase I trials when combined with checkpoint inhibitors resulted in an objective response rate of 24%.([27])”
Background
Holistic analytical characterization and risk assessment of residual host cell protein impurities in an active pharmaceutical ingredient synthesized by biocatalysts
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“…to pose a significant immunogenicity risk due to their low abundance level (<20 ng/mg in API for those with high in silico risk) and the low dose of MK‐1454 (10–3000 µg; Harrington et al., 2018), these materials have not been assessed for immunotoxicity in animal studies or clinical trials.”
BackgroundMethod
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“Results from the use ofMK-1454 were initially reported at the European Society ofMedical Oncology Meeting in 2018 (NCT03010176).(60) Treatment related adverse events occurred in 83% of monotherapy patients as well as 82% of STING agonist plus anti-PD-1 therapy treated patients.”
Method
IL-38 blockade induces anti-tumor immunity by abrogating tumor-mediated suppression of early immune activation
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“STING MK-1454 1 NCT03010176 [82] Combination MK-1454 (ulveostinag) + pembrilizumab vs.”
Activation of dendritic cells by targeted DNA: a potential addition to the armamentarium for anti-cancer immunotherapy
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“In a phase 1 study, MK-1454 in combination with pembrolizumab had encouraging efficacy and an acceptable safety profile in patients with advanced solid tumors or lymphoma [57].”
Background
Intratumoural immunotherapy: activation of nucleic acid sensing pattern recognition receptors
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High levels of tumor cell-intrinsic STING signaling are associated with increased infiltration of CD8+ T cells in dMMR/MSI-H gastric cancer
Kanoda, R., Nakajima, S., Fukai, S., Saito, M., Saito, K., Suzuki, H., Kikuchi, T., Nirei, A., Okayama, H., Mimura, K., et al. (2024) · Scientific Reports · doi:10.1038/s41598-024-71974-3 · Cited by 15
“Furthermore, a combination therapy using MK-1454 and anti-PD-1 antibody showed a 24% response rate with reductions in the size of both target-injected and noninjected lesions (83% median) in advanced solid tumors 27 .”
Inhibitory Microenvironment Remodeling Enhances STING Activation for Solid Tumor Immunotherapy
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“Early clinical trials of small-molecule STING agonists (for example, Adu-S100 and MK-1454) have shown moderate clinical response but significant patient morbidities (grade 3/4 adverse effects) 11,12 .”
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“Another intratumoral STING agonist MK-1454 had minimal response when used as monotherapy in patients with advanced solid tumors, but 24% in combination with pembrolizumab [58].”
Background
STING Agonists in Head and Neck Squamous Cell Carcinoma
Wallington, D. G., Contessa, J. N., & Hayman, T. J. (2022) · The Cancer Journal · doi:10.1097/ppo.0000000000000620 · Cited by 12
Nanomaterials Application for STING Pathway-Based Tumor Immunotherapy
Zhao, W., Tang, X., Qin, Y., Wang, X., Zhong, K., Gong, N., & Li, T. (2025) · International Journal of Nanomedicine · doi:10.2147/ijn.s535460 · Cited by 11
Harnessing cGAS‐STING Pathway for Cancer Immunotherapy: From Bench to Clinic
Lee, D., Huntoon, K. M., Kang, M., Lü, Y., Gallup, T. D., Jiang, W., & Kim, B. Y. S. (2022) · Advanced Therapeutics · doi:10.1002/adtp.202200040 · Cited by 10
Novel Modifications and Delivery Modes of Cyclic Dinucleotides for STING Activation in Cancer Treatment
Lu, Y., Li, Z., Zhu, X., Zeng, Q., Liu, S., & Guan, W. (2025) · International Journal of Nanomedicine · doi:10.2147/ijn.s503780 · Cited by 11
“55,101 In the bargain, combining with other treatment modalities or being the payload agents for novel delivery systems provides new ideas for CDN drugs to activate the STING pathway and related cancer immunotherapy.”
Potential role of cGAS/STING pathway in regulating cancer progression
Dhanisha, S. S., & Guruvayoorappan, C. (2022) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2022.103780 · Cited by 11
Targeting DNA Damage Response and Immune Crosstalk in Cancer: Mechanistic Insights and Therapeutic Opportunities
Mărcuț, L. F., Brata, R. D., Barb, A. C., Manole, A., Stef, D. G., Dumitru, C. Ș., Zara, F., & Pătrașcu, R. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms262311271 · Cited by 11
“First-generation cyclic dinucleotides (CDNs) such as ADU-S100 (MIW815) [141] and MK-1454 [142] demonstrated potent local interferon induction but suffered from poor bioavailability and dose-limiting inflammation in phase I trials.”
Nanoparticle targeting cGAS-STING signaling in disease therapy
Zhou, L., Huang, Y., Wu, Y., & Tang, S. (2024) · Nano Research · doi:10.1007/s12274-024-6714-x · Cited by 11
Potentiating intratumoral therapy with immune checkpoint inhibitors: shifting the paradigm of multimodality therapeutics
Nelson, B. E., Naing, A., Fu, S., Sheth, R. A., Murthy, R., & Piha-Paul, S. A. (2024) · Immuno-Oncology Technology · doi:10.1016/j.iotech.2024.101040 · Cited by 10
Molecular and Radiological Features of Microsatellite Stable Colorectal Cancer Cases With Dramatic Responses to Immunotherapy
Keenan, B. P., Loon, K. V., Khilnani, A. D., Fidelman, N. A., Behr, S. C., Atreya, C. E., & Oh, D. Y. (2021) · Anticancer Research · doi:10.21873/anticanres.15080 · Cited by 10
Self-citation
Molecular mechanisms and therapeutic strategies of cGAS-STING pathway in liver disease: the quest continues
Fan, Y., Dong, Z., Wu, Y., & Wen, H. (2025) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1692365 · Cited by 10
Activation of Stimulator of Interferon Genes (STING): Promising Strategy to Overcome Immune Resistance in Prostate Cancer
Alnukhali, M., Altabbakh, O., Farooqı, A. A., Pollack, A. S., Daunert, S., Deo, S. K., & Tao, W. (2024) · Current Medicinal Chemistry · doi:10.2174/0109298673273303231208071403 · Cited by 9
Small molecule innate immune modulators in cancer therapy
Goswami, A., Goyal, S., Khurana, P., Singh, K., Deb, B., & Kulkarni, A. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1395655 · Cited by 10
Interferon-induced factor 16 is essential in metastatic melanoma to maintain STING levels and the immune responses upon IFN-γ response pathway activation
Kobayashi, Y., Bustos, M. A., Hayashi, Y., Yu, Q., & Hoon, D. S. �. (2024) · Journal for ImmunoTherapy of Cancer · doi:10.1136/jitc-2024-009590 · Cited by 9
Immunotherapy in Advanced NSCLC Without Driver Mutations: Available Therapeutic Alternatives After Progression and Future Treatment Options
Leal, J. L., & John, T. (2022) · Clinical Lung Cancer · doi:10.1016/j.cllc.2022.08.009 · Cited by 9
Type I interferons: One stone to concurrently kill two birds, viral infections and cancers
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Chemotherapy in synergy with innate immune agonists enhances T cell priming for checkpoint inhibitor treatment in pancreatic cancer
Niu, N., Li, K., Wang, J.-K., et al. (2025) · Biomarker Research · doi:10.1186/s40364-024-00721-7 · Cited by 8
“MK-1454, a synthetic CDN, was tested as monotherapy or in combination with anti-PD-1 antibody (α-PD-1) pembrolizumab for the treatment of advanced solid tumors (NCT03010176, NCT04220866) [15].”
An imaging-guided self-amplifying photo-immunotherapeutic nanoparticle for STING pathway activation and enhanced cancer therapy
Chen, Q., Yu, H., Li, N., Zhang, H., Tan, M., Liu, W., Zheng, M., Hu, Y., Cheng, L., Chen, Y., et al. (2025) · Journal of Nanobiotechnology · doi:10.1186/s12951-025-03536-2 · Cited by 9
“However, the clinical application of STING agonists is hindered by their poor metabolic and circulatory stability, low cellular uptake efficiency, and insufficient efficacy, which collectively limit their effective intracellular delivery [11, 12].”
Targeting DNA Damage Response-Mediated Resistance in Non-Small Cell Lung Cancer: From Mechanistic Insights to Drug Development
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“Additionally, Wang et al. suggested that inhibiting FLOT1 in combination with STING agonists, which promote both innate and adaptive immunity, could potentially rescue the suboptimal effects of STING agonist monotherapy [32,35].”
Systemic administration of STING agonist promotes myeloid cells maturation and antitumor immunity through regulating hematopoietic stem and progenitor cell fate
Xu, T., Dai, J., Tang, L., Sun, L., Si, L., & Guo, J. (2023) · Cancer Immunology Immunotherapy · doi:10.1007/s00262-023-03502-7 · Cited by 10
“In 2018, it was reported that single-agent treatment with MK-1454 did not achieve a partial or complete response in patients with advanced solid tumors or lymphomas, and the objective response rate of MK-1454 plus anti-PD-1 antibody Keytruda was less than 30% [46].”
Background
Engaging Pattern Recognition Receptors in Solid Tumors to Generate Systemic Antitumor Immunity
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Next-Generation Immunotherapy Approaches in Melanoma
Buchanan, T., Amouzegar, A., & Luke, J. J. (2021) · Current Oncology Reports · doi:10.1007/s11912-021-01104-z · Cited by 9
Lipid nanoparticles delivering constitutively active STING mRNA as a novel anti-cancer therapeutic approachPreprint
Liu, W., Alameh, M., Yang, J. F., Xu, J. R., Lin, P. J. C., Tam, Y. K., Weissman, D., & You, J. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.01.08.475499 · Cited by 8
“However, clinical trials of these STING agonists did not show beneficial results [39,40].”
Background
Design of an Oral STING Agonist through Intramolecular Hydrogen Bond Ring Mimicking to Achieve Complete Tumor Regression
Zhao, H., Tao, J., Zhang, L., Li, Q., He, M., Wen, B., Liu, Z., Myatt, H., & Sun, D. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00296 · Cited by 9
Research advances in immune agonists and their nanoparticles for enhancing the immunotherapeutic efficacy of PD-1 inhibitors in malignancies
Xia, R., Liang, J., Ma, J., Du, X., Ma, L., Han, X., Wang, Y., Qin, J., & Yan, L. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2025.1618903 · Cited by 7
Novel targeted therapies and immunological strategies for breast cancer treatment
Mussa, A., Hamid, M. A. M., Talib, M., Ehinnou, I. B., Bragoli, A. J., Hajissa, K., Mokhtar, N. F., Mohamud, R., Al-Hatamleh, M. A. I., & Hassan, R. (2026) · Biochemical Pharmacology · doi:10.1016/j.bcp.2026.117929 · Cited by 10
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“Other strategies to boost the immune response against KRAS-mutant cancers include STING agonists (ADU-S100, MK-1454) [101,144,145], as well as CAR-T cells (adoptive T-cell transfer) [146] and mRNA vaccine technology [147].”
Background
Personalised Medicine and the Potential Role of Electrospinning for Targeted Immunotherapeutics in Head and Neck Cancer
O’Meara, C. H., Nguyen, T. V., Jafri, Z., Boyer, M. J., Shonka, D. C., & Khachigian, L. M. (2023) · Nanomaterials · doi:10.3390/nano14010006 · Cited by 8
Cyclic diguanylate analogues: Facile synthesis, STING binding mode and anti-tumor immunity delivered by cytidinyl/cationic lipid
Sun, X., Yu, X., Zhao, Y., Xing, L., Na, L., Chen, Z., Xiao, Z., Dai, H., Yu, J., Long, S., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.115053 · Cited by 8
Novel immune‐modulating drugs for advanced head and neck cancer
Chen, T.-H., Chang, P. M., & Yang, M. (2019) · Head & Neck · doi:10.1002/hed.25929 · Cited by 8
“Twenty-five patients were enrolled in the MK-1454/pembrolizumab combination group; there were no CRs, but 6 of 25 patients achieved a PR, and 6 had SD.(17) Both injected tumors and other metastatic tumors showed regression in responders, with a median 83% reduction in tumor size.”
BackgroundInfluential

Authors: Harrington, K. J., Brody, J., Ingham, M., Strauss, J., Cemerski, S., Wang, M., Tse, A., Khilnani, A., Marabelle, A., & Golan, T.
Affiliations: Institute of Cancer Research (GB)
Mount Sinai Hospital (US)
Columbia University Irving Medical Center (US)
Mary Crowley Cancer Research Center (US)
Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
Institut Gustave Roussy (FR)
Sheba Medical Center (IL)
ORCID: Harrington, K.J.
Brody, J.
Strauss, J.
Khilnani, A.
Marabelle, A.
Golan, T.
Venue: Annals of Oncology
Publisher: Elsevier BV
Published: 2018-10
Volume: 29
Pages: viii712
ISSN: 0923-7534 (ISSN-L)
DOI: 10.1093/annonc/mdy424.015
OpenAlex: W2898106814
Cited by: 280
References: 0
Citations by year: 2026: 34 · 2025: 50 · 2024: 37 · 2023: 28 · 2022: 42 · 2021: 50 · 2020: 18 · 2019: 20
FWCI: 9.57
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 483 d)
Locations: Annals of Oncology (publishedVersion)
Funders: Amgen
Pfizer
AstraZeneca
Topics: Life Sciences › Immunology and Microbiology › Immunology › interferon and immune responses
Health Sciences › Medicine › Oncology › Cancer Immunotherapy and Biomarkers
Life Sciences › Immunology and Microbiology › Immunology › Immunotherapy and Immune Responses
Keywords: STING agonist, cyclic dinucleotides, pembrolizumab, immune checkpoint inhibitor combination, advanced solid tumors, lymphoma, antitumor immunity, intratumoral administration

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Preliminary results of the first-in-human (FIH) study of MK-1454, an agonist of stimulator of interferon genes (STING), as monotherapy or in combination with pembrolizumab (pembro) in patients with advanced solid tumors or lymphomas

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