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1m
A Study of Maintenance Treatment With Fluzoparib in gBRCA/PALB2 Mutated Pancreatic Cancer Whose Disease Has Not Progressed on First Line Platinum-Based Chemotherapy (clinicaltrials.gov)
P3, N=5, Terminated, Jiangsu HengRui Medicine Co., Ltd. | N=136 --> 5 | Recruiting --> Terminated; Sponsor R & D Strategy Adjustment
Enrollment change • Trial termination • Metastases
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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BRCA2 mutation • BRCA1 mutation • PALB2 mutation
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AiRuiYi (fluzoparib)
2ms
A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors (clinicaltrials.gov)
P1/2, N=306, Recruiting, Risen (Suzhou) Pharma Tech Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open • Combination therapy • Metastases
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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PIK3CA mutation
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paclitaxel • Loqtorzi (toripalimab-tpzi) • capecitabine • Irene (pyrotinib) • fulvestrant • AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib)
2ms
New P3 trial • Combination therapy • Metastases
|
BRCA (Breast cancer early onset)
|
gemcitabine • paclitaxel • AiTan (rivoceranib) • capecitabine • Halaven (eribulin mesylate) • AiRuiYi (fluzoparib) • Navelbine oral (vinorelbine tartrate oral)
2ms
New P2 trial • Metastases
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AiRuiYi (fluzoparib) • adebrelimab (SHR-1316)
3ms
Case report of penile squamous cell carcinoma continuous treatment with BRCA2 mutation. (PubMed, World J Surg Oncol)
This is the first report of penile cancer with BRCA2 mutation, receiving a combination treatment with olaparib and experiencing a benefit for 9 months. This case underscores the pivotal role of BRCA2 in influencing treatment response in PSCC, providing valuable insights into the application of targeted therapies in managing recurrent PSCC with BRCA2 alterations. This elucidation establishes a crucial foundation for further research and clinical considerations in similar cases.
Journal • Tumor mutational burden • BRCA Biomarker • PARP Biomarker • PD(L)-1 Biomarker • IO biomarker
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TMB (Tumor Mutational Burden) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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BRCA2 mutation • BRCA1 mutation
|
Keytruda (pembrolizumab) • Opdivo (nivolumab) • Lynparza (olaparib) • Yervoy (ipilimumab) • Focus V (anlotinib) • AiRuiYi (fluzoparib)
3ms
Safety and Pharmacokinetics of Fluzoparib in Healthy Subjects and Those With Impaired Kidney Function (clinicaltrials.gov)
P1, N=24, Completed, Jiangsu HengRui Medicine Co., Ltd. | Not yet recruiting --> Completed | Trial completion date: Oct 2022 --> Dec 2023 | Trial primary completion date: Oct 2022 --> Dec 2023
Trial completion • Trial completion date • Trial primary completion date
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AiRuiYi (fluzoparib)
3ms
New P1/2 trial • Combination therapy • Metastases
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
|
PIK3CA mutation
|
paclitaxel • Loqtorzi (toripalimab-tpzi) • capecitabine • Irene (pyrotinib) • fulvestrant • AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib)
4ms
Maintenance Therapy After Platinum-containing Chemotherapy in Patients With Recurrent Ovarian Cancer (clinicaltrials.gov)
P3, N=37, Not yet recruiting, The First Affiliated Hospital of Xiamen University
New P3 trial
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AiTan (rivoceranib) • AiRuiYi (fluzoparib)
5ms
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1. (PubMed, J Med Chem)
The currently approved PARP inhibitors include olaparib, niraparib, rucaparib, talazoparib, fuzuloparib, and pamiparib. The present review introduces the necessity for research on the development of selective PARP-1 inhibitors from the perspective of structural and functional mechanisms of PARP-1 inhibition. A review of recently reported selective PARP-1 inhibitors provides the foundation for exploring novel strategies for designing selective PARP-1 inhibitors from the perspective of structure-activity relationships combined with computer simulations.
Review • Journal
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PARP2 (Poly(ADP-Ribose) Polymerase 2)
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Lynparza (olaparib) • Talzenna (talazoparib) • Zejula (niraparib) • Rubraca (rucaparib) • Partruvix (pamiparib) • AiRuiYi (fluzoparib)
5ms
Fluzoparib and Abiraterone in the preSurgery Treatment of Prostate Cancer: FAST Trial (clinicaltrials.gov)
P2, N=34, Active, not recruiting, Fudan University | Recruiting --> Active, not recruiting | Trial completion date: May 2023 --> Dec 2023
Enrollment closed • Trial completion date
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abiraterone acetate • prednisone • AiRuiYi (fluzoparib)
5ms
New P2 trial
|
AiTan (rivoceranib) • AiRuiYi (fluzoparib)
5ms
New P4 trial
|
MUC16 (Mucin 16, Cell Surface Associated)
|
AiTan (rivoceranib) • AiRuiYi (fluzoparib)
6ms
Enrollment open
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
HER-2 negative
|
tamoxifen • Verzenio (abemaciclib) • letrozole • anastrozole • exemestane • AiRuiYi (fluzoparib) • goserelin acetate
6ms
Development and validation of a sensitive LC-MS/MS method for the assay of four PARP inhibitors in human plasma and its application in ovarian cancer patients. (PubMed, J Pharm Biomed Anal)
In this study, we established and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) based method to simultaneously quantify the four frequently prescripted PARP inhibitors, namely niraparib, olaparib,fluzoparib, and pamiparib, in ovarian cancer. The mean plasma concentrations (±SD) of niraparib and olaparib were 424.76 (±228.35) ng/mL and 1760.47 (±1739.69) ng/mL, respectively. The validated LC-MS/MS method allows the convient and efficient determination of four PARP inhibitors' exposure levels in ovarian cancer patients.
Journal • BRCA Biomarker • PARP Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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Lynparza (olaparib) • Zejula (niraparib) • Partruvix (pamiparib) • AiRuiYi (fluzoparib)
6ms
PARP inhibitors: A review of the pharmacology, pharmacokinetics, and pharmacogenetics. (PubMed, Semin Oncol)
Currently, four agents, namely olaparib, rucaparib, niraparib, and talazoparib, have obtained approval in the United States and Europe. Additionally, this review briefly covers veliparib, a PARP inhibitor under development, and two recently approved PARP inhibitors in China, fuzuloparib and pamiparib. Although significant progress has been made in understanding PARP inhibitors, there are several unanswered questions that remain, necessitating further research across a broader spectrum of cancer types within this evolving class of anticancer agents.
PK/PD data • Review • Journal • PARP Biomarker
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PARP2 (Poly(ADP-Ribose) Polymerase 2)
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Lynparza (olaparib) • Talzenna (talazoparib) • Zejula (niraparib) • Rubraca (rucaparib) • veliparib (ABT-888) • Partruvix (pamiparib) • AiRuiYi (fluzoparib)
6ms
AN PROSPECTIVE; SINGLE-ARM; PHASE Ⅱ STUDY OF ALTERNATING REGIMENS OF FLUZOPARIB AND ORAL ETOPOSIDE MAINTENANCE THERAPY; IN NEWLY DIAGNOSED ADVANCED OVARIAN CANCER: FARE TRIAL (IGCS 2023)
A current therapy option for advanced OC patients is debulking surgery; followed by platinum-based chemotherapy ± bevacizumab; followed by maintenance therapy with bevacizumab or monotherapy with PARP inhibitors. Primary endpoint is progressionfree survival (PFS). Current Trial Status: Trial in progress: there are no available results at the time of submission, and there are no available conclusions at the time of submission.
Clinical • BRCA Biomarker • PARP Biomarker • Metastases
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HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset)
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HRD • BRCA mutation
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Avastin (bevacizumab) • etoposide oral • AiRuiYi (fluzoparib)
6ms
Adebrelimab Combined With Fuzuloparib in the Treatment of Patients With Recurrent Platinum-resistant Ovarian Cancer. (clinicaltrials.gov)
P2, N=37, Recruiting, Fujian Cancer Hospital | Not yet recruiting --> Recruiting | Initiation date: May 2023 --> Aug 2023
Enrollment open • Trial initiation date
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HRD (Homologous Recombination Deficiency)
|
AiRuiYi (fluzoparib) • adebrelimab (SHR-1316)
7ms
New P2 trial • Metastases
|
BRCA (Breast cancer early onset)
|
AiRuiKa (camrelizumab) • AiRuiYi (fluzoparib)
7ms
A phase 1 trial of fuzuloparib in combination with apatinib for advanced ovarian and triple-negative breast cancer: efficacy, safety, pharmacokinetics and germline BRCA mutation analysis. (PubMed, BMC Med)
Fuzuloparib plus apatinib had acceptable safety in patients with advanced OC or TNBC. Fuzuloparib 100 mg bid plus apatinib 500 mg qd was established as the RP2D. With the promising clinical activity observed, this combination is warranted to be further explored as a potential alternative to chemotherapy.
P1 data • PK/PD data • Journal • Combination therapy • BRCA Biomarker • PARP Biomarker • Metastases
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BRCA (Breast cancer early onset)
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BRCA mutation
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AiTan (rivoceranib) • AiRuiYi (fluzoparib)
7ms
New P2 trial • Combination therapy • Metastases
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
BRCA wild-type
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Avastin (bevacizumab) • AiRuiYi (fluzoparib)
7ms
A Clinical Study of Chemoradiotherapy Sequential Fluzoparib in Pan-solid Tumors (clinicaltrials.gov)
P2, N=120, Not yet recruiting, Chongqing University Cancer Hospital
New P2 trial
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EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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EGFR mutation • ALK mutation • ROS1 mutation
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AiRuiKa (camrelizumab) • capecitabine • AiRuiYi (fluzoparib)
8ms
Enhanced efficacy of combined fluzoparib and chidamide targeting in natural killer/T-cell lymphoma. (PubMed, Ann Hematol)
In vivo, this combined regimen also showed synergistic antitumor effects in xenograft mouse models. The combination of fluzoparib and chidamide showed synergistic effects against NKTCL both in vitro and in vivo and deserves further exploration in clinical trials.
Journal • BRCA Biomarker • PARP Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • RAD51 (RAD51 Homolog A)
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BRCA2 mutation • BRCA1 mutation
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Epidaza (chidamide) • AiRuiYi (fluzoparib)
8ms
P2 data • Journal
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • FGFR (Fibroblast Growth Factor Receptor) • PARP2 (Poly(ADP-Ribose) Polymerase 2) • PARP3 (Poly(ADP-Ribose) Polymerase Family Member 3)
|
Avastin (bevacizumab) • sorafenib • Focus V (anlotinib) • thalidomide • AiRuiYi (fluzoparib)
9ms
Fluzoparib in Combination With Camrelizumab and Temozolomide in Advanced Melanoma (clinicaltrials.gov)
P1/2, N=50, Not yet recruiting, Peking University Cancer Hospital & Institute
New P1/2 trial • Combination therapy • Metastases
|
SF3B1 (Splicing Factor 3b Subunit 1)
|
SF3B1 mutation
|
temozolomide • AiRuiKa (camrelizumab) • AiRuiYi (fluzoparib)
9ms
Enrollment open • Trial initiation date • Metastases
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
AiRuiYi (fluzoparib) • Ankeda (bevacizumab biosimilar)
9ms
New P2 trial • Combination therapy • Metastases
|
BRCA (Breast cancer early onset)
|
AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib)
10ms
Preoperative Moderately Fractionated IMRT for Locally Extremity or Trunk Sarcoma (clinicaltrials.gov)
P2, N=100, Recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences
New P2 trial
|
AiRuiYi (fluzoparib)
10ms
New P2 trial • Metastases
|
EGFR (Epidermal growth factor receptor) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TP53 (Tumor protein P53) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
|
TP53 mutation • ALK positive • TP53 R175H • TP53 R248Q • TP53 Y220C • TP53 R273H • TP53 R273C
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AiTan (rivoceranib) • AiRuiYi (fluzoparib) • adebrelimab (SHR-1316)
10ms
New P1/2 trial • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
HER-2 negative • ER negative • PGR negative
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AiRuiKa (camrelizumab) • AiRuiYi (fluzoparib) • Airui'en (rezvilutamide)
11ms
Fluzoparib in Patients With Metastatic Non-clear Cell Renal Cell Carcinoma (clinicaltrials.gov)
P2, N=1, Completed, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School | Recruiting --> Completed | N=37 --> 1 | Trial completion date: Mar 2022 --> Jun 2023 | Trial primary completion date: Mar 2022 --> Jun 2023
Trial completion • Enrollment change • Trial completion date • Trial primary completion date • Metastases
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AiRuiYi (fluzoparib)
11ms
New P2 trial • Combination therapy • Metastases
|
AiRuiYi (fluzoparib)
11ms
New P3 trial
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
HER-2 negative
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tamoxifen • Verzenio (abemaciclib) • letrozole • anastrozole • exemestane • AiRuiYi (fluzoparib) • goserelin acetate
12ms
Itraconazole interferes in the pharmacokinetics of fuzuloparib in healthy volunteers. (PubMed, Cancer Chemother Pharmacol)
The CYP3A4 inhibitor itraconazole has a significant influence on the PK behavior of fuzuloparib, suggesting to avoid using strong CYP3A4 inhibitors simultaneously with fuzuloparib. If it is necessary to use a strong CYP3A4 inhibitor, fuzuloparib would be discontinued and be restored to the original dose and frequency of administration after 5-7 half lives of CYP3A4 inhibitor stopped.
PK/PD data • Journal
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AiRuiYi (fluzoparib) • itraconazole
12ms
PARP INHIBITORS ARE EFFECTIVE IN NATURAL KILLER/T CELL LYMPHOMA VIA THE EXPRESSION OF LMO2 (EHA 2023)
Finally, the combination of fluzoparib and cisplatin exhibited significant synergistic effects both in vitro and in vivo . In summary, we found that PARPis exerted an anti-lymphoma effect in NKTCL, and the underlying mechanisms may be "synthetic lethality-like" via LMO2 expression. Moreover, LMO2 may be a novel indicator for drug sensitivity and prognosis in NKTCL. These findings offer a foundation for the clinical application of PARPis and provide certain implications for the clinical management of NKTCL.
PARP Biomarker
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LMO2 (LIM Domain Only 2)
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LMO2 overexpression
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cisplatin • AiRuiYi (fluzoparib)
1year
Neoadjuvant Fluzoparib in Germline BRCA-mutated Three-negative Breast Cancer Breast Cancer (clinicaltrials.gov)
P2, N=60, Recruiting, The First Affiliated Hospital with Nanjing Medical University
New P2 trial
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset)
|
BRCA2 mutation • BRCA1 mutation
|
paclitaxel • cyclophosphamide • epirubicin • AiRuiYi (fluzoparib)
1year
New P2 trial
|
HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • CHEK2 (Checkpoint kinase 2) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • BARD1 (BRCA1 Associated RING Domain 1)
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HER-2 negative
|
AiRuiKa (camrelizumab) • albumin-bound paclitaxel • AiRuiYi (fluzoparib)
1year
New P2 trial • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
ER positive • HR positive • HER-2 negative • PGR positive
|
fulvestrant • AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib)
1year
New P2 trial • Metastases
|
BRCA1 (Breast cancer 1, early onset) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • RAD51D (RAD51 paralog D)
|
HRD
|
irinotecan • AiRuiYi (fluzoparib)
1year
Enrollment open
|
HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor) • CD8 (cluster of differentiation 8) • FOXC1 (Forkhead Box C1)
|
Herceptin (trastuzumab) • carboplatin • Perjeta (pertuzumab) • AiRuiKa (camrelizumab) • Irene (pyrotinib) • albumin-bound paclitaxel • cyclophosphamide • letrozole • epirubicin • trastuzumab rezetecan (SHR-A1811) • AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib) • goserelin acetate • adebrelimab (SHR-1316)
over1year
Cost-effectiveness of fuzuloparib compared to routine surveillance, niraparib and olaparib for maintenance treatment of patients with germline BRCA1/2 mutation and platinum-sensitive recurrent ovarian carcinoma in China. (PubMed, Front Pharmacol)
One-way sensitivity analysis revealed that the results were sensitive to the PFS and the price of medicines. Fuzuloparib was less cost-effective for patients with germline BRCA1/2 mutation and platinum-sensitive recurrent OC compared to olaparib, but was superior to niraparib from the Chinese healthcare systems perspective.
Journal • HEOR • BRCA Biomarker • PARP Biomarker • Cost-effectiveness • Cost effectiveness
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
BRCA2 mutation • BRCA1 mutation
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Lynparza (olaparib) • Zejula (niraparib) • AiRuiYi (fluzoparib)
over1year
SNF Platform Study of HR+/ HER2-advanced Breast Cancer (clinicaltrials.gov)
P2, N=140, Recruiting, Fudan University | Not yet recruiting --> Recruiting
Enrollment open • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
ER positive • HR positive • HER-2 amplification • HER-2 negative • PGR positive
|
sorafenib • everolimus • AiRuiKa (camrelizumab) • AiTan (rivoceranib) • capecitabine • albumin-bound paclitaxel • fulvestrant • exemestane • trastuzumab rezetecan (SHR-A1811) • AiRuiYi (fluzoparib) • AiRuiKang (dalpiciclib) • goserelin acetate • famitinib (SHR 1020)
over1year
New P2 trial • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 negative
|
AiRuiKa (camrelizumab) • AiRuiYi (fluzoparib)