Drug Database
TR

trastuzumab (HS 022 / HS022 / anruize)

✓ Approved

BioRay Pharmaceutical · ERBB2 · Monoclonal Antibodies

What is trastuzumab?

trastuzumab is a monoclonal antibodies developed by BioRay Pharmaceutical. It is approved for therapeutic indications via injectable (others) or intravenous (iv).

Drug Profile

Brand NamesHS 022, HS022, anruize
CompanyBioRay Pharmaceutical
Drug ClassMonoclonal Antibodies, Antibody
Molecular TargetERBB2
RouteInjectable (Others), Intravenous (IV)
StatusApproved
Sources: ClinicalTrials.gov, BioRay Pharmaceutical

Mechanism of Action

Molecular Targets

trastuzumab acts on 1 molecular target:

ERBB2erb-b2 receptor tyrosine kinase 2 (NEU, CD340)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

trastuzumab is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Breast cancer✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Gastric cancer✓ Approved

Related Research Articles

PubMedClinical cancer research : an official journal of the American Association for Cancer Research2026-07-17

Targetable S100-RAGE signaling mediates intrinsic trastuzumab deruxtecan resistance in metastatic breast cancer.

Dong Wenjuan W, Wang Shiruo S, Chan Bill B, Vasquez Matthew M et al.

Trastuzumab deruxtecan (T-DXd) has improved outcomes in metastatic breast cancer; however, a substantial subset of patients experience early lack of clinical benefit that is not reliably predicted by routine clinicopathologic variables. In an institutional cohort of 109 T-DXd-treated metastatic lesions, HER2 expression level, ER/PR status, Ki-67 index, and metastatic site were not significantly associated with response, highlighting the need to define mechanistic determinants of intrinsic resistance. We performed spatial transcriptomic and proteomic profiling using NanoString GeoMx Digital Spatial Profiling on pretreatment bone, brain, and soft-tissue metastases from patients with clinical benefit (response) versus early progression (resistance) on T-DXd. Tumor (PanCK⁺) and immune (CD45⁺) compartments were analyzed to link tumor architecture and region-resolved signaling states with therapeutic response. Candidate resistance pathways were functionally evaluated in HER2-positive breast cancer cell lines and in vivo metastasis models treated with T-DXd alone or combined with the RAGE inhibitor TTP488. Spatial proteogenomics revealed recurrent upregulation of S100 family alarmins in resistant tumor regions, associated with activation of a RAGE-centered pro-survival signaling program characterized by ERK, AKT, and STAT3 phosphorylation. Pharmacologic RAGE inhibition enhanced T-DXd-induced apoptosis, restored drug sensitivity in vitro, and significantly reduced metastatic burden in lung and brain metastasis models. Spatial proteogenomics identifies a conserved S100-RAGE-driven survival state coupled to immune-excluded tumor architecture as a mechanism of intrinsic T-DXd resistance across metastatic niches. Targeting this pathway with an orally available RAGE antagonist restores T-DXd responsiveness and offers an immediately translatable strategy to overcome resistance in metastatic breast cancer.

PMID 42467226
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PubMedLung cancer (Amsterdam, Netherlands)2026-07-17

Interstitial lung disease in patients treated with antibody-drug conjugates: a review.

Petrelli Fausto F, Dottorini Lorenzo L, D'Alessio Andrea A, Tarantini Francesco F et al.

Antibody-drug conjugates (ADCs) are increasingly used across solid tumors, including lung cancer, but drug-related interstitial lung disease (ILD)/pneumonitis has emerged as a clinically relevant and potentially fatal toxicity. This narrative review summarizes evidence from clinical trials, pooled analyses, pharmacovigilance studies, mechanistic investigations, and consensus recommendations on the epidemiology, pathophysiology, diagnosis, risk factors, and management of ADC-related ILD. ILD has been most extensively characterized with trastuzumab deruxtecan (T-DXd), for which pooled analyses report an incidence of approximately 10-15%, a median onset of 5-6  months, and a fatal-event rate of about 2.2%. However, pulmonary toxicity is not restricted to HER2-directed ADCs and has also been reported with deruxtecan-based agents targeting TROP2 and HER3, as well as with non-deruxtecan ADCs. Pharmacovigilance data from 1,277 cases showed that ILD, pneumonitis, and acute respiratory distress syndrome accounted for 40.6%, 27.9%, and 7.6% of pulmonary events, respectively; acute respiratory distress syndrome had the earliest onset and highest case-fatality. Mechanistic data support antigen-independent, dose-dependent ADC uptake by alveolar macrophages through Fcγ receptors, followed by intracellular payload release and cytokine-mediated lung injury. Risk is influenced by ADC type, payload, dose, age, pre-existing lung disease, and concomitant pulmonary-toxic therapies. ADC-related ILD is a class-relevant toxicity requiring baseline risk assessment, serial high-resolution chest computed tomography, prompt treatment interruption, grade-based corticosteroid therapy, and multidisciplinary management. Structured surveillance and early intervention may substantially reduce severe and fatal outcomes.

PMID 42462539
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PubMedFrontiers in immunology2026-07-16

Immune checkpoint inhibitors plus trastuzumab and chemotherapy for the treatment of advanced HER2-positive gastric and gastroesophageal junction cancers: a systematic review and meta-analysis.

Zhan Hongjie H, Zhang Hongbo H, Tian Caijuan C, Liu Pengfei P et al.

HER2-positive gastric and gastroesophageal junction (GEJ) cancers have poor prognosis despite standard trastuzumab-based chemotherapy. Immune checkpoint inhibitors (ICIs) may enhance therapeutic efficacy when combined with trastuzumab. A systematic review and meta-analysis were conducted following PRISMA guidelines. PubMed, Cochrane Library, Embase, and Scopus were searched up to December 29, 2025. Studies evaluating ICIs plus trastuzumab and chemotherapy versus trastuzumab-based therapy alone were included. Kaplan-Meier curves were digitized using WebPlotDigitizer and reconstructed to individual participant data (IPD). Pooled survival outcomes, objective response rate (ORR), disease control rate (DCR), and safety were analyzed. Six studies including 1,097 patients were included. ICIs plus trastuzumab and chemotherapy significantly improved median progression-free survival (10.4 vs. 8.27 months; HR 0.6951, p<0.0001) and overall survival (20.4 vs. 17.2 months; HR 0.8104, p=0.004) compared with control. ORR (OR 1.85, p<0.00001) and DCR (OR 2.46, p=0.006) were also superior. Grade ≥3 adverse events were similar between groups. ICIs combined with trastuzumab and chemotherapy improve survival and response rates in HER2-positive gastric/GEJ cancers with manageable toxicity, supporting their integration into treatment strategies. https://www.crd.york.ac.uk/prospero/, identifier CRD420261280958.

PMID 42459656
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PubMedESMO open2026-07-16

Next-generation precision oncology in microsatellite stable colorectal cancer: integrated targeting beyond RAS and RAF.

Bartolini M M, Algaze S S, Lenz H-J HJ

The therapeutic landscape of colorectal cancer (CRC) has evolved with the identification of molecular subtypes, including mismatch repair-deficient/microsatellite instability-high, POLE mutations, RAS/BRAF alterations, and HER2 amplification, enabling use of precision therapies and immune checkpoint inhibitors for selected populations. However, most microsatellite-stable (MSS) tumors remain resistant due to tumor heterogeneity, adaptive resistance, and an immunosuppressive tumor microenvironment (TME). Advances in molecular profiling, spatial biology, and immune characterization have revealed vulnerabilities beyond canonical signaling, facilitating novel strategies such as antibody-drug conjugates (ADCs), bispecific antibodies, DNA damage response (DDR) targeting, TME-directed therapies, cellular therapies, and epigenetic modulation. HER2-directed ADCs, notably trastuzumab deruxtecan, have shown clinically meaningful activity in HER2-positive metastatic CRC, providing proof of concept for ADC-based therapy. Additional targets under investigation include CEACAM5, LGR5, EGFR, HER3, MET, B7-H3, and CDH17. Bispecific antibodies and co-stimulatory agonists are being developed to overcome antigen heterogeneity and pathway redundancy, with the EGFR-MET bispecific antibody amivantamab showing initial clinical efficacy. Moreover, next-generation immune checkpoint inhibitors and multitarget combinations aim to reinvigorate T-cell responses in MSS tumors. Early chimeric antigen receptor T-cell studies targeting CEA and GUCY2C demonstrate feasibility and manageable toxicity, although tumor-intrinsic and TME barriers persist. Emerging strategies increasingly focus on modulating the TME to enhance immune infiltration and effector function, targeting CCR8, TGF-β, adenosine, CSF1R, CXCR1/2, STING, and CD47. DDR and epigenetic therapies offer additional opportunities to sensitize resistant tumors. Integrated, multidimensional biomarker approaches and artificial intelligence-driven interpretation of tumor and TME features are expected to guide personalized therapy, anticipate resistance, and broaden the benefit of targeted and immune-based interventions in CRC.

PMID 42462280
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PubMedClinical pharmacokinetics2026-07-16

Transitioning Therapeutic Antibodies in Oncology from Intravenous to Hyaluronidase-Facilitated Subcutaneous Administration.

Xu Xu Steven XS

Intravenous (IV) infusion remains the predominant delivery route for oncology monoclonal antibodies, but it requires prolonged chair time and substantial infusion-unit resources. Hyaluronidase-facilitated subcutaneous (SC) formulations aim to shorten administration (minutes vs hours), improve convenience, and potentially expand outpatient or home-based delivery, while preserving exposure, efficacy, and safety. We conducted a narrative review of published clinical studies, major congress presentations, trial registries, and Food and Drug Administration (FDA)/European Medicines Agency (EMA) regulatory documents describing development of hyaluronidase-facilitated SC formulations for seven oncology antibodies (trastuzumab, rituximab, daratumumab, atezolizumab, nivolumab, pembrolizumab, and amivantamab). We extracted evidence on formulation strategy, pharmacokinetic (PK) bridging, efficacy comparability, safety/immunogenicity, and regulatory pathways supporting IV→SC approval. Across programs, PH20-based recombinant hyaluronidases, including human hyaluronidase PH20 (rHuPH20) and berahyaluronidase alfa, transiently depolymerize SC hyaluronan, enabling delivery of multi-milliliter injections and high fixed doses. Development strategies converged on PK-anchored bridging, typically targeting non-inferior SC/IV geometric-mean ratios for both initiation and maintenance exposure (e.g., cycle-1 area under the curve [AUC]/average plasma concentration [Cavg] and minimum plasma concentration [Cmin]/trough concentration [Ctrough]), supported by population PK to ensure covariate coverage. We highlight a pragmatic evolution in trial design: earlier conversions often paired PK with direct clinical activity confirmation in sensitive settings, whereas more recent programs increasingly use prespecified PK non-inferiority as the confirmatory backbone with efficacy as supportive reassurance-enabling use of an approved SC formulation across multiple indications. In pivotal bridging trials, SC regimens generally met or exceeded exposure targets and demonstrated efficacy consistent with IV comparators (treatment effects clustering around unity; Δ ≈ 0; hazard ratio/relative risk ≈ 1). Safety profiles were broadly similar; SC administration was associated with fewer administration-related reactions for several agents, while injection-site reactions were usually mild. Immunogenicity, including anti-hyaluronidase antibodies, did not show consistent clinically meaningful effects on PK or outcomes. Hyaluronidase-facilitated IV→SC conversion has become a reproducible, model-informed, PK-driven development paradigm. By synthesizing study-design choices, formulation pathways, and extrapolation logic across seven approved antibodies-including the recent IO and targeted-therapy wave-this review builds upon a previously described clinical bridging concept and provides a comprehensive updated overview including the most recently approved products, with a practical framework to guide future IV→SC transitions in oncology.

PMID 42461495
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PubMedExpert opinion on emerging drugs2026-07-15

Emerging biological drugs for the treatment of metastatic HER2+ gastroesophageal adenocarcinomas.

Rogers Jane E JE, Horak Ashley A, Kroll Alicia A, Ajani Jaffer A JA

Advanced gastroesophageal adenocarcinomas (GEAs) continue to represent an area in need of new drug development. Targeting human epidermal growth factor receptor-2 (HER2) in GEAs has been standard since 2010 and continues to be an area of further development. Trastuzumab became the first targeted agent approved for GEA. Added to front-line fluoropyrimidine plus platinum chemotherapy in HER2+ metastatic disease, trastuzumab improved survival. Pembrolizumab was approved in HER2 positive GEA for those PD-L1 positive with modest benefit. Since trastuzumab's approval, other anti-HER2 agents had limited impact until 2021 with the FDA approval of trastuzumab deruxtecan. Trastuzumab deruxtecan represents an option after trastuzumab-based therapy fails. Other agents are currently being investigated. With the abundance of anti-HER2 therapies in the investigative pipeline, understanding key resistance mechanisms seen in HER2+ GEA will be the path to success. Technology advancements to provide real time precision medicine are likely in the coming years. We hope these advancements can help combat and/ or understand some of the intratumoral heterogeneity, HER2 expression changes, and tumor microenvironment resistance pathways seen in HER2+ GEA.

PMID 42454937
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