Liporaxel (paclitaxel oral) / Dae Hwa, HaiHe Biopharma - LARVOL DELTA

Phase III of oral paclitaxel (DHP107) vs intravenous paclitaxel in HER2-negative recurrent or metastatic breast cancer (mBC): Primary analysis of a multinational optimal trial (NCT03315364). (ASCO 2025) - P2/3 | "Clinical Trial Registration Number: NCT03315364 The abstract will be released to the public on May 22, 2025 at 5:00 PM EDT"

Metastases • P3 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Daehwa Pharm eyes China, Europe as oral chemo matches IV paclitaxel in phase 2/3 breast cancer trial (Korea Biomedical Review) - P2/3 | N=549 | OPTIMAL (NCT03315364) | Sponsor: Daehwa Pharmaceutical Co., Ltd | "Results from a phase 2/3 study, released Wednesday, showed that Liporaxel matched the efficacy of injectable paclitaxel as a first-line treatment for recurrent or metastatic HER2-negative breast cancer...The 582-patient, multi-country trial met its primary endpoint, demonstrating non-inferiority in progression-free survival (PFS) in the per-protocol set (PPS) population. Median PFS was 10.02 months with Liporaxel versus 8.54 months for the IV formulation. Secondary endpoints—including overall survival (OS), objective response rate (ORR), disease control rate (DCR), time to treatment failure (TTF), and quality of life (EQ-5D-3L)—also showed a non-inferior trend. The company plans to submit label expansion applications in Korea and China within the first half of the year, with Haihe Biopharma leading the process in China."

China filing • Korea filing • P2/3 data • Breast Cancer • HER2 Negative Breast Cancer

Paclitaxel oral solution versus paclitaxel injection as a second-line therapy in advanced gastric cancer: A randomized, open-label, non-inferiority phase 3 trial. (ASCO-GI 2025) - P3 | "Paclitaxel oral solution (Liporaxel), the world's first successfully developed oral formulation, is an alternative. Paclitaxel oral solution demonstrated non-inferiority in PFS and superiority in OS compared to paclitaxel IV, with clinically manageable and favorable safety profile, supporting paclitaxel oral solution as a second-line treatment option for gastric cancer"

Clinical • Head-to-Head • Metastases • P3 data • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

An open-label, multicenter, randomized, non-inferior Phase III trial comparing the efficacy and safety of paclitaxel oral solution (RMX3001DHP107) versus paclitaxel injection (Taxol) in second-line treatment of patients with advanced gastric cancer (Haihe Biopharma Press Release) - P3 | N=400 | CTR20190050 | Sponsor: Daehwa Pharmaceutical Co., Ltd. | "Median progression-free survival assessed by BIRC was 3.02 months (95% confidence interval [CI]: 2.69, 3.71) in the oral group and 2.89 months (95% CI: 2.53, 3.48) in the injection group, demonstrating non-inferiority conclusion (HR 0.894, 95% CI: 0.719, 1.112, p=0.311). Median overall survival (as of February 15, 2023) was 9.13 months (95% CI: 7.72, 10.97) in the oral group and 6.54 months (95% CI: 5.75, 7.26) in the injection group, showing superiority with an absolute 2.59-month survival improvement (HR 0.770, 95.5% CI: 0.635, 0.934, p=0.006). Paclitaxel oral solution was clinically manageable."

P3 data • Gastric Cancer

Daehwa Pharm’s Liporaxel wins Chinese approval to treat gastric cancer (Korea Biomedical Review) - "Daehwa Pharm...announced on Thursday that it has received marketing authorization from China's National Medical Products Administration (NMPA) for Liporaxel Sol. (Liporaxel), an oral paclitaxel for the treatment of gastric cancer....Liporaxel eliminates the need for pre-treatment and the three-hour dosing time associated with conventional paclitaxel intravenous (IV) therapy. Clinical trials have demonstrated improved outcomes for gastric cancer patients using Liporaxel compared to IV therapy, particularly regarding hair loss and peripheral neuropathy....The company said its ongoing phase 3 breast cancer MRCT study in Korea, China, and three countries in Eastern Europe is expected to be completed by the end of 2024. Then, the company will be able to submit additional indication applications in Korea and China in 2025."

China approval • China filing • Korea filing • Trial completion date • Breast Cancer • Gastric Cancer

Food Effect on Pharmacokinetics and Safety of DHP107 (Liporaxel®) FEEL Study (clinicaltrials.gov) - P1 | N=25 | Completed | Sponsor: Daehwa Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Completed

Metastases • Trial completion • Breast Cancer • Head and Neck Cancer • Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor

OPTIMAL: Oral Paclitaxel Trial In Recurrent and Metastatic Breast Cancer As 1st Line Therapy (clinicaltrials.gov) - P2/3 | N=549 | Active, not recruiting | Sponsor: Daehwa Pharmaceutical Co., Ltd. | Trial completion date: Mar 2024 ➔ Dec 2025

Metastases • Trial completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor

Paclitaxel oral solution versus paclitaxel injection as second-line therapy in advanced gastric cancer: A randomized, open-label, non-inferiority phase 3 trial. (ASCO 2024) - "Safer and more convenient paclitaxel oral solution (Liporaxel), the world's first oral formulation, has been initially approved in Korea for treatment of gastric cancer. The study showed statistical non-inferiority of paclitaxel oral solution in PFS and statistically significant and clinically meaningful improvement in OS as compared to paclitaxel IV, with clinically manageable safety profile, supporting paclitaxel oral solution as second-line treatment option for patients with gastric cancer."

Clinical • Head-to-Head • Metastases • P3 data • Anemia • Gastric Cancer • Gastrointestinal Cancer • Hematological Disorders • Immunology • Oncology • Pain • Solid Tumor

GIST Oral Paclitaxel(Liporaxel) (clinicaltrials.gov) - P2 | N=28 | Not yet recruiting | Sponsor: Asan Medical Center

New P2 trial • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

Daehwa Pharm's Liporaxel Sol. wins orphan drug designation in Europe (Korea Biomedical Review) - "Daehwa Pharm, a Kosdaq-listed drugmaker, said Friday it received orphan drug designation (ODD) from the European Medicines Agency (EMA) for Liporaxel Solution, an oral paclitaxel, for the second-line treatment of gastric cancer on Feb. 26. Daehwa explained that the orphan drug designation for Liporaxel Solution will allow the company to receive benefits, such as a shorter review period for new drug applications in Europe, reduced fees and taxes for marketing authorization applications, and exclusivity for 10 years after approval."

Orphan drug • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

OPERA: Oral Paclitaxel Efficacy Safety and PK in Recurrent and Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=72 | Completed | Sponsor: Daehwa Pharmaceutical Co., Ltd. | Unknown status ➔ Completed

Metastases • Trial completion • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor • HER-2

Anti-cancer effects of DHP107 on canine mammary gland cancer examined through in-vitro and in-vivo mouse xenograft models. (PubMed, BMC Vet Res) - "Our results suggest that paclitaxel may have anti-cancer effects on CMGC through cell cycle arrest, induction of apoptosis, and anti-angiogenesis. This study could provide a novel approach to treat CMGC."

Journal • Preclinical • Breast Cancer • Oncology • Oral Cancer • CCND1 • PECAM1

OPTIMAL: Oral Paclitaxel Trial In Recurrent and Metastatic Breast Cancer As 1st Line Therapy (clinicaltrials.gov) - P2/3 | N=549 | Active, not recruiting | Sponsor: Daehwa Pharmaceutical Co., Ltd. | Unknown status ➔ Active, not recruiting | Trial completion date: Mar 2022 ➔ Mar 2024 | Trial primary completion date: Dec 2020 ➔ Jan 2024

Enrollment closed • Metastases • Trial completion date • Trial primary completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor

Oral paclitaxel formulations forming in situ mucoadhesive lipidic mesophases and particles in GI tract (ACS-Fall 2023) - "Liporaxel, a peroral paclitaxel formulation approved for the treatment of gastric cancer in Korea, contains monoacylglycerols, triacylglycerols, polysorbate 80 and 1 w/w% of paclitaxel. Differential scanning calorimetry and small-angle x-ray diffraction studies were also performed to investigate the physical characteristics of the oral paclitaxel formulations. Distribution of paclitaxel in blood after oral administration of paclitaxel formulations at 5 mL/kg dose in ICR mice (A) and the cryo-transmission electron microscopy of formulation G6 in excess water (B)"

Gastric Cancer • Gastrointestinal Cancer • Gastrointestinal Disorder • Oncology • Solid Tumor

Phase II study of DHP107 oral paclitaxel compared to IV paclitaxel in patients with HER2-negative recurrent or metastatic breast cancer (MBC): Opera (NCT03326102) (ESMO 2022) - P2, P2/3 | "Conclusions The oral paclitaxel, DHP107 showed comparable efficacy and a differential safety including less neuropathy compared to IV ptx in pts with MBC. The ongoing OPTIMAL Phase III will enroll 556 subjects with MBC in Korea, China and Europe to test non-inferiority of DHP107 to IV ptx (NCT03315364)."

Clinical • P2 data • Breast Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

Chinese regulator accepts Daehwa Pharm’s sales application for oral paclitaxel drug (Korea Biomedical Review) - "Daehwa Pharmaceutical said Wednesday that it had been notified of the acceptance of the application for new drug approval for Liporaxel/RMX3001, oral paclitaxel (DHP107/RMX3001) drug, from China’s National Medical Products Administration. The indication of Liporaxel/RMX3001 seeking the Chinese permit is the secondary treatment for patients with advanced gastric cancer. Daehwa Pharmaceutical, along with its Chinese partner Haihe Biopharma, conducted phase 3 clinical trials in China, applied for approval based on them, and received the notification of acceptance."

Non-US regulatory • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Retrospective analysis of efficacy and safety of oral paclitaxel for treatment of various cancers in dogs (2017-2021). (PubMed, Vet Med Sci) - "Based on the observed responses in certain types of cancers and the minimal adverse events, the study findings supported the efficacy and safety of oral paclitaxel administration in dogs. Thus, oral paclitaxel could play a role in the management of cancer in dogs."

Journal • Retrospective data • Oncology

A 64-Year-Old Woman With Advanced Endometrial Carcinoma - Episode 6: Advanced Endometrial Carcinoma: Systemic Therapy & Patient Prognosis (Targeted Oncology) - "Robert L. Coleman, MD, FACOG, FACS: Prognosis is something that’s regularly updated. When we started this case, this patient was diagnosed as having a grade 2, stage IB endometrioid microsatellite-stable endometrial cancer. She had surgery and evidence of no metastatic disease by the assessment and was treated with vaginal cuff brachytherapy. Our estimation of her prognosis at that stage was quite good. We would have expected that her potential for recurrence was probably on the order of 20% or 25%, and unfortunately, she fell into that category. Her prognosis then would be reevaluated at the first recurrence. At that point, she had relatively limited disease, but it was definitely present."

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Phase II study of DHP107 (oral paclitaxel) in the first-line treatment of HER2-negative recurrent or metastatic breast cancer (OPTIMAL study). (PubMed, Ther Adv Med Oncol) - P2/3 | "DHP107 showed promising efficacy and acceptable tolerability in this phase II study and is currently being investigated in the OPTIMAL phase III study (NCT03315364). This trial was registered with ClinicalTrials.gov identifier: NCT03315364."

Clinical • Journal • P2 data • Breast Cancer • Febrile Neutropenia • Gastric Cancer • Gastrointestinal Cancer • Hematological Disorders • HER2 Breast Cancer • HER2 Negative Breast Cancer • Immunology • Infectious Disease • Neutropenia • Oncology • Oral Cancer • Pain • Septic Shock • Solid Tumor • Triple Negative Breast Cancer • HER-2

Neutrophil-lymphocyte ratio (NLR) as an important prognostic factor for paclitaxel as a second line chemotherapy in advanced gastric cancer (AGC): Results from phase 3 DREAM study (ESMO 2018) - P3; "Recently, the DREAM phase 3 study (NCT01839773) have demonstrated that the efficacy and safety of DHP107, an oral paclitaxel, is comparable to those of intravenous (i.v.) paclitaxel. The current study demonstrates that low NLR is correlated with better treatment outcomes for both oral and intravenous paclitaxel as a second-line chemotherapy in AGC."

Biomarker • Clinical • P3 data • Gastric Cancer

Phase II study of DHP107 oral paclitaxel in first-line, HER2 negative recurrent/metastatic breast cancer (OPTIMAL study, NCT03315364) (ESMO 2019) - P2/3; "Based on confirmed PR (n = 16/33, 48.5%), DHP107 demonstrated adequate efficacy with manageable toxicity in the first line HER2 negative recurrent/metastatic breast cancer patients. Phase III trial in breast cancer is ongoing in Korea and China. Legal entity responsible for the study: Daehwa Pharmaceuticals."

Clinical • P2 data

[VIRTUAL] Pharmacokinetic evaluation of an oral paclitaxel DHP107 (Liporaxel®) in patients with recurrent or metastatic breast cancer (MBC): Phase II study (OPERA, NCT03326102) (SABCS 2020) - P2 | "Compared to previous phase I PK results in Korean patients, C max and AUC parameters were similar after dosing with DHP107, demonstrating no clinically significant differences between Asian and Caucasian patients. Safety and efficacy will be evaluated in the ongoing OPERA and OPTIMAL studies."

Clinical • P2 data • PK/PD data • Breast Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

A phase II study to evaluate the efficacy, safety and pharmacokinetics of DHP107 (Liporaxel®, oral paclitaxel) compared to IV paclitaxel in patients with recurrent or metastatic breast cancer: OPERA (NCT03326102) (SABCS 2019) - P2; "Target Accrual: The first subject was enrolled in July 2018 and recruitment is ongoing. Enrollment of 72 evaluable subjects is expected to complete in Q2 2020."

Clinical • P2 data • PK/PD data • HER2 • MRI

[VIRTUAL] [OPTIMAL 3] A phase III trial to evaluate the efficacy and safety of DHP107 (Liporaxel, oral paclitaxel) compared to Taxol (IV paclitaxel) as first line therapy in patients with recurrent or metastatic HER2 negative breast cancer (BC) (NCT03315364). (ASCO 2020) - P2/3 | "Final results of this study will be announced by the end of 2022. Research Funding: DAEHWA Pharmaceutical Co,.Ltd."

Clinical • P3 data • Breast Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

Tissue pharmacokinetics of DHP107, a novel lipid-based oral formulation of paclitaxel, in mice and patients by positron emission tomography. (PubMed, Clin Transl Sci) - "Systemic exposures after administration of a DHP107 therapeutic dose were comparable with those in previous studies. PET using radioisotope-labeled drug candidates is useful for drug development and can provide valuable information that can complement plasma PK data, particularly in early phase clinical trials."

Journal • PK/PD data • Preclinical • Breast Cancer • Oncology • Solid Tumor