Irene (pyrotinib) / Jiangsu Hengrui Pharma, HLB Bio Group - LARVOL DELTA

Pyrotinib combined with dalpiciclib in the treatment of refractory advanced HER2-positive gastric cancer or solid tumors: Safety and efficacy results from a phase Id trial (ESMO Asia 2025) - P1 | "Pyrotinib combined with dalpiciclib showed acceptable safety profile and encouraging efficacy in refractory advanced HER2-positive GC, even for patients pretreated with anti-HER2 ADCs."

Clinical • Metastases • Gastric Cancer • Oncology • Solid Tumor • HER-2

A multicenter real-world study on survival analysis of pyrotinib in HER2-positive metastatic breast cancer (ESMO Asia 2025) - "The updated analysis indicates that pyrotinib may serve as a promising therapeutic option for HER2-positive MBC with manageable toxicity in real-world settings. Survival outcomes remain under evaluation with extended follow-up."

Clinical • Metastases • Real-world • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Pertuzumab versus pyrotinib in combination with trastuzumab and taxanes for first-line (1L) treatment of patients with HER2–positive metastatic breast cancer (HER2+MBC): A multicenter real-world study (ESMO Asia 2025) - "Background: The CLEOPATRA study established taxane+trastuzumab+pertuzumab(THP)as the 1L standard for HER2+ MBC over a decade ago. The recent PHILA study showed that docetaxel+trastuzumab+pyrotinib (an irreversible pan-HER receptor tyrosine kinase inhibitor ) (THPy) significantly prolonged progression-free survival (PFS)versus placebo group, establishing it as a viable 1L option in China.Given limited comparative evidence, this real-world study aimed to evaluate the effectiveness of THP and THPy in HER2+ MBC patients and identify potential beneficiary populations for each regimen. Patients who were treated with THP or THPy as a 1L treatment between January 2018 and March 2025 were included in this multicenter real-world study... Compared with the THP ,THPy significantly improved PFS in patients with untreated HER2+MBC. Notably, THPy demonstrated superior survival benefits specifically in subgroups with:premenopausal status, ECOG PS 0, de novo stage IV disease, previous..."

Clinical • Combination therapy • Metastases • Real-world • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Clinical efficacy and safety of pyrotinib as the first-line treatment of HER2-positive advanced breast cancer in Xinjiang Uygur Autonomous Region of China. (PubMed, Transl Cancer Res) - "Pyrotinib showed good antitumor activity in the treatment of patients with HER2-positive advanced breast cancer and displayed a degree of efficacy in patients with brain metastases. The main adverse reaction was diarrhea, which was mostly low to moderate in severity, and the incidence of high-grade AEs was generally low, with controllable toxicity."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • Women's Health • HER-2

Pyrotinib or placebo in combination with trastuzumab and docetaxel for untreated HER2-positive metastatic breast cancer: long-term survival results from the phase 3 PHILA study (SABCS 2025) - P3 | "Although cross-over was not allowed, the proportions of pts receiving pyrotinib, trastuzumab, pertuzumab, or anti-HER2 antibody-drug conjugate (incl. T-DM1, T-DXd, SHR-A1811) after study treatment discontinuation in each group were 18.5% vs. 51.9%, 26.3% vs. 25.6%, 15.5% vs. 14.0%, and 22.6% vs. 28.0%, respectively... The long-term analysis confirms that the previously observed improvements in OS and PFS with PyroHT compared to HT in the first-line treatment of HER2-positive metastatic breast cancer were maintained after 45.5 months of median follow-up. Notably, with PyroHT, 5-year OS rate remained at 66% and nearly 30% of pts remained progression-free at 5 years. PyroHT treatment delayed time to onset of brain metastasis."

Clinical • Combination therapy • Metastases • P3 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

A New Hope: Dual Human Epidermal Growth Factor Receptor 2 Blockade and Chemotherapy in Human Epidermal Growth Factor Receptor 2-Amplified Colorectal Cancer - A Case Report and Literature Review. (PubMed, Case Rep Oncol) - "Dual HER2-targeted therapy combined with chemotherapy is a promising strategy for HER2-positive mCRC patients with good performance status. This approach warrants validation in large-scale clinical trials to confirm its efficacy."

Journal • Colorectal Cancer • Oncology • Solid Tumor • HER-2

Development and validation of a two-dimensional liquid chromatography method for therapeutic drug monitoring of pyrotinib in human plasma. (PubMed, Front Pharmacol) - "The developed 2D-LC analytical method not only demonstrates good precision, accuracy, recovery, and stability, but also is simple, rapid, feasible, and practical for TDM. It can be used for the concentration monitoring of pyrotinib in clinic, providing more scientific evidence for clinical practice."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Gut Microbiota and Diarrhea in Breast Cancer Patients Receiving Pyrotinib (clinicaltrials.gov) - P=N/A | N=60 | Not yet recruiting | Sponsor: Hubei Cancer Hospital

New trial • Breast Cancer • Oncology • Solid Tumor

Pyrotinib plus capecitabine with or withoutradiotherapyin patients with HER2-positive metastatic breast cancer and brain metastases: Amulticenter, retrospective-prospective, real-world study in China (Post-PERMEATE) (SABCS 2025) - P=N/A | "Therefore, future studies should further elucidate the characteristics of patients most likely to benefit from specific systemic-local treatment combinations and enabling personalized therapeutic strategies for HER2-positive breast cancer patients with BMs. These findings warrant prospective clinical investigation.Research Sponsor: None."

Metastases • Real-world • Real-world evidence • Retrospective data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Efficacy of cross-line therapy with anti-HER2 TKI in HER2-positive MBC: a multicenter real-world study (SABCS 2025) - "Importantly, patients who switched from lapatinib to pyrotinib had a significantly longer PFS2 compared to those who continued pyrotinib in the second-line setting (mPFS: 7.0 vs. 4.1 months, HR 0.523, 95%CI 0.298 - 0.917, P < 0.001). This study indicated that cross-line anti-HER2 TKI therapy confers sustained PFS benefits in HER2-positive MBC. Notably, patients with longer frontline PFS and those who switched TKI agents exhibited superior survival outcomes in subsequent treatment lines. Further prospective studies are warranted to confirm these findings."

Clinical • Real-world • Real-world evidence • Breast Cancer • HER2 Positive Breast Cancer

Dalpiciclib Plus Pyrotinib Plus Letrozole for Patients with Estrogen Receptor-Positive and HER2-Positive Metastatic Breast Cancer (DAPLET) (SABCS 2025) - P2 | "Standard metastatic regimens combining trastuzumab-based HER2-targeted therapy with chemotherapy show limited efficacy in this subtype. This chemotherapy-free, trigeminy-targeted regimen demonstrated promising antitumor activity and manageable toxicity in first or second line HER2+ER+ metastatic breast cancer. The data supported this regimen as a potential alternative to standard chemotherapy-based approaches in this subtype. Efficacy of this regimen needs to be further evaluated in Simon stage II."

Clinical • Metastases • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER • HER-2

Neoadjuvant pyrotinib, trastuzumab, dalpiciclib, and exemestane in triple-positive breast cancer: a multicenter phase II trial (SABCS 2025) - "The NA-PHER2 study demonstrated the potential benefit of a chemotherapy-free regimen, trastuzumab, pertuzumab, palbociclib, and fulvestrant, in TPBC...In the phase II MUKDEN 01 trial, pyrotinib combined with dalpiciclib and letrozole showed promise in TPBC, though efficacy remains suboptimal... This chemotherapy-free, quadruple-targeted neoadjuvant regimen demonstrated promising activity and manageable toxicity in early-stage TPBC. These data support further evaluation of this regimen as a potential alternative to standard chemotherapy-based neoadjuvant approaches in TPBC."

Clinical • P2 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER • PGR

A real-world study of pyrotinib as neoadjuvant therapy for HER2-positive breast cancer (SABCS 2025) - "Background: A double-blind, randomized Phase 3 clinical study, PHEDRA, met its primary endpoint with a significantly higher tpCR rate than placebo in patients treated with pyrotinib, trastuzumab, and docetaxel in HER2-positive early or locally advanced breast cancer (41.0% vs. 22.0%, unilateral P< 0.0001). In this real-world study, neoadjuvant pyrotinib- containing regimens showed promising efficacy and safety in patients with HER2-positive breast cancer, further verify its effectiveness and safety in the real world."

Clinical • Real-world • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Efficacy and safety of disitamab vedotin combined with pyrotinib as neoadjuvant therapy for HER2-positive breast cancer: a phase II trial (SABCS 2025) - "Post-surgery, adjuvant therapy (epirubicin 90 mg/m² + cyclophosphamide 600 mg/m² Q3W, cycles 5-8) was administered, followed by maintenance therapy (cycles 9-22): trastuzumab + pertuzumab for pCR patients, T-DM1 or trastuzumab + pertuzumab for non-pCR patients. This first neoadjuvant study combining HER2-ADC and TKI demonstrated a chemo-free neoadjuvant regimen with high efficacy. The safety profile was manageable, with hepatic toxicity requiring longer follow-up. These results support randomized evaluation against standard chemotherapy-containing regimens."

Clinical • P2 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Trastuzumab Combined with Pyrotinib and Capecitabine as Postoperative Adjuvant Therapy in Non-Pathological Complete Response HER2-Positive Early Breast Cancer Following Neoadjuvant Therapy: A Multicenter Phase II Study (SABCS 2025) - P2 | "For patients with HER2-positive early breast cancer who did not achieve pCR (residual invasive tumor >1 cm or lymph node metastasis) following neoadjuvant therapy, the combination of pyrotinib, trastuzumab and capecitabine as postoperative adjuvant therapy appears to improve prognosis. The overall safety profile of the regimen was acceptable, with no new safety signals identified. Primary prophylaxis with loperamide effectively reduced the incidence of grade ≥3 diarrhea during adjuvant therapy with pyrotinib."

Clinical • P2 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Assessment of the efficacy of various neoadjuvant anti-HER2 targeted therapies combined with chemotherapy for HER2-positive breast cancer in the real-world setting and development of a predictive model for pathological complete response. (PubMed, Front Oncol) - "The efficacy of NAT regimens containing trastuzumab plus pertuzumab (HP) and trastuzumab plus pyrotinib (HPy) was compared. Both HP and HPy combined with chemotherapy can be considered as optional NAT regimens for HER2-positive BC. The nomogram incorporating common clinical indicators provides a basis for clinicians to predict NAT efficacy at an earlier stage."

Journal • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • HER-2

Phase II Clinical Study of Pyrotinib in First-line Treatment of Primary HER2-amplified/Mutated Advanced Non-small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=18 | Recruiting | Sponsor: Peking Union Medical College Hospital | N=45 ➔ 18 | Trial completion date: Dec 2025 ➔ Dec 2026 | Trial primary completion date: Dec 2023 ➔ Dec 2026

Enrollment change • Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2

Pyrotinib Plus Trastuzumab as an Effective Later-Line Therapeutic Strategy for HER2-Positive Metastatic Colorectal Cancer: Results from a Phase II Study. (PubMed, Drug Des Devel Ther) - "Pyrotinib plus trastuzumab demonstrates clinically meaningful efficacy and a manageable safety profile in heavily pretreated HER2-positive metastatic colorectal cancer. These findings support advancing this regimen as a potential alternative in refractory HER2-positive mCRC, particularly in the RAS/BRAF wild-type subgroup."

Clinical • Journal • P2 data • Colorectal Cancer • Fatigue • Oncology • Solid Tumor • BRAF • HER-2 • KRAS

HER2-targeted therapy combined with multidisciplinary management in advanced gallbladder cancer: a case report with 90-month survival. (PubMed, Front Oncol) - "The patient achieved a prolonged period of disease stability, who was treated with various anti-HER2 targeted therapy, such as trastuzumab combined with pyrotinib and HER2-targeted antibody-drug conjugate (ADC). Dynamic CA199 levels paralleled the treatment efficacy. This report underscores the significance of molecular profiling-guided personalized therapy and integrated multidisciplinary management in the treatment of biliary tract cancers."

Journal • Biliary Cancer • Biliary Tract Cancer • Gallbladder Cancer • Oncology • Solid Tumor • CA 19-9

Non-intravenous chemotherapy-sparing triplet of dalpiciclib/pyrotinib/endocrine therapy… (PLEASURABLE phase 2 trial) (ABC8 2025) - No abstract available

P2 data • Oncology

CORIN-PYRA: Continuous or Intermittent Pyrotinib for HER2-positive Advanced Breast Cancer (clinicaltrials.gov) - P2 | N=186 | Recruiting | Sponsor: Wenjin Yin | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor

Clinical Efficacy and Safety of Targeted Therapies for HER2 Mutant Advanced or Metastatic Non-Small Cell Lung Cancer: A Systematic Literature Review (ISPOR-EU 2025) - "Only two trials - both on pyrotinib - used progression-free survival (PFS) as the primary outcome and included HER2-mutated and/or HER2-amplified metastatic NSCLC... HER2-targeted therapies in advanced NSCLC have shown potential for rapid and durable responses in HER2-mutant populations, though efficacy varies considerably and comparative evidence remains limited."

Clinical • Metastases • Review • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2

Combined treatment of inetetamab plus pyrotinib and vinorelbine in managing advanced HER2-positive breast cancer patients (ILLUMINE): a multicenter, retrospective, real-world study. (PubMed, Transl Breast Cancer Res) - "No severe TAAEs were observed during the investigation. The triple regimen of inetetamab plus pyrotinib and vinorelbine exhibited promising therapeutic effects and was tolerable for participants with HER2-positive ABC."

Journal • Real-world evidence • Retrospective data • Breast Cancer • Hematological Disorders • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Leukopenia • Neutropenia • Oncology • Solid Tumor • HER-2

An LC-MS/MS method for simultaneous quantification of pyrotinib, docetaxel and paclitaxel in human plasma and its application to therapeutic drug monitoring. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "With imatinib as internal standard, one-step deproteinization approach with acetonitrile was applied to extract analytes and purify specimens. The therapeutic drug monitoring results showed that the plasma concentration of pyrotinib, docetaxel and paclitaxel varied significantly among individuals. Therapeutic drug monitoring for pyrotinib, docetaxel and paclitaxel is essential for individualized treatment to ensure efficacy and safety."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Treatment beyond progression and rechallenge with pyrotinib in HER2-positive metastatic breast cancer and brain metastases: a multicenter real-world study. (PubMed, Ther Adv Med Oncol) - "Among patients with BMs before pyrotinib re-treatment, the median PFS for pyrotinib re-treatment was 7.2 months, and the median OS was 25.2 months. Pyrotinib TBP and pyrotinib rechallenge both demonstrate potential benefits for patients with HER2-positive MBC, including those with BM."

Journal • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2