| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized (frommouse) |
| Target | PD-1 |
| Clinical data | |
| Other names | AK105, penpulimab-kcqx |
| MedlinePlus | a625068 |
| License data | |
| Routes of administration | Intravenous |
| Drug class | Antineoplastic agent |
| ATC code |
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| Legal status | |
| Legal status | |
| Identifiers | |
| CAS Number | |
| PubChem SID | |
| IUPHAR/BPS | |
| DrugBank | |
| UNII | |
| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C6434H9922N1718O2012S46 |
| Molar mass | 145008.92 g·mol−1 |
Penpulimab is ahumanized monoclonal antibody used for the treatment ofcancer.[1] It targets theprogrammed cell death protein 1 (PD-1) receptor.[1][2] It is developed byAkeso.[1]
Penpulimab was approved for medical use in China in August 2021,[3] and in the United States in April 2025.[4]
In the United States, penpulimab isindicated for the treatment of non-keratinizingnasopharyngeal carcinoma.[1][4]
In August 2021, penpulimab received its first approval in China for the treatment of adults with relapsed or refractory classicHodgkin lymphoma who have undergone at least second-line chemotherapy.[3]
In January 2023, the National Medical Products Administration of China approved penpulimab in combination with chemotherapy for the first-line treatment of locally advanced or metastatic squamousnon-small cell lung cancer.[5]
The most common adverse effects associated with penpulimab include:
Penpulimab binds to the PD-1 receptor onT cells, preventing interaction with its ligands, PD-L1 and PD-L2.[6] This blockade restores T-cell-mediated immune responses against tumor cells. The antibody has been engineered with modifications to its Fc region to eliminate Fcγ receptor binding and Fc-mediated effector functions, reducing the risk of immune-related adverse effects such as antibody-dependent cellular cytotoxicity (ADCC) or phagocytosis.[7]
Penpulimab demonstrates a slower dissociation rate from the PD-1 receptor compared to other PD-1 inhibitors, resulting in higher receptor occupancy and enhanced T-cell activity.[6] This property is attributed to its unique binding interactions with the glycosylated N58 residue on the BC loop of the PD-1 receptor.[6]
Penpulimab is produced using recombinant DNA technology in Chinese hamster ovary cells. It has been designed with an IgG1 backbone and modified Fc regions to minimize immune-related side effects.[7]
The efficacy of penpulimab withcisplatin orcarboplatin andgemcitabine was evaluated in study AK105-304 (NCT04974398), a randomized, double-blind, multi-center trial in 291 participants with recurrent or metastatic nasopharyngeal carcinoma who had not received previous systemic chemotherapy for recurrent or metastatic disease.[4] Participants were randomized (1:1) to receive either penpulimab with cisplatin or carboplatin and gemcitabine, followed by penpulimab, orplacebo with cisplatin or carboplatin and gemcitabine, followed by placebo.[4]
The efficacy of single-agent penpulimab was evaluated in study AK105-202 (NCT03866967), an open-label, multi-center, single-arm trial conducted in a single country.[4] The trial included a total of 125 participants with unresectable or metastatic non-keratinizing nasopharyngeal carcinoma who had disease progression afterplatinum-based chemotherapy and at least one other line of therapy.[4] Participants received penpulimab until disease progression or unacceptable toxicity, for a maximum of 24 months.[4]
In March 2025, penpulimab, was approved by theNational Medical Products Administration in China for the first-line treatment of recurrent or metastaticnasopharyngeal cancer in combination with chemotherapy.[8]
In April 2025, the USFood and Drug Administration (FDA) approved penpulimab-kcqx with cisplatin or carboplatin and gemcitabine for the first-line treatment of adults with recurrent or metastatic non-keratinizing nasopharyngeal carcinoma.[4] The FDA also approved penpulimab-kcqx as a single agent for adults with metastatic non-keratinizing nasopharyngeal carcinoma with disease progression on or after platinum-based chemotherapy and at least one other prior line of therapy.[4] The FDA granted the application for penpulimabfast track,breakthrough therapy, andorphan drug designations.[4]
Penpulimab is theinternational nonproprietary name.[9]
Penpulimab is sold under the brand name安尼可 (Anike) in China.[3]
Penpulimab is being studied in various clinical trials to evaluate its efficacy and safety for additional cancer indications, including nasopharyngeal carcinoma,[10][11] non-small-cell lung cancer, and other solid tumors.[3]
This article incorporates text from this source, which is in thepublic domain.
