Toripalimab (Monograph)

Brand name: Loqtorzi
Drug class: Antineoplastic Agents

Medically reviewed by Drugs.com on Mar 10, 2025. Written by ASHP.

Introduction

Antineoplastic agent; humanized anti-programmed-death receptor-1 (anti-PD-1) monoclonal antibody.

Uses for Toripalimab

Nasopharyngeal Carcinoma

In combination with cisplatin and gemcitabine as first-line treatment of adults with metastatic or with recurrent, locally advanced nasopharyngeal carcinoma (NPC).

As a single agent for treatment of adults with recurrent unresectable or metastatic NPC with disease progression on or after a platinum-containing chemotherapy.

Designated an orphan drug by FDA for treatment of NPC.

ASCO guidelines for recurrent and metastatic head and neck cancers recommend toripalimab, camrelizumab, or tislelizumab, with gemcitabine and cisplatin, as first line treatment for patients with recurrent or metastatic NPC. ASCO guidelines also state PD-1 inhibitors may be offered to patients with recurrent or metastatic NPC who have progressed following platinum-based therapy.

Toripalimab Dosage and Administration

General

Pretreatment Screening

Perform pregnancy testing in females of reproductive potential.
Assess baseline liver enzymes, creatinine, and thyroid function.

Patient Monitoring

Assess liver enzymes, creatinine, and thyroid function periodically during treatment.
Monitor patients for hyperglycemia or other signs and symptoms of diabetes.
Monitor patients for signs and symptoms of infusion-related reactions.
Closely monitor patients for signs and symptoms of immune-mediated adverse reactions during treatment.
Closely monitor patients who undergo allogeneic hematopoietic stem cell transplantation for evidence of transplant-related complications.

Dispensing and Administration Precautions

If chemotherapy is also administered on the same day as toripalimab-tpzi, administer toripalimab prior to chemotherapy.

Administration

IV Administration

Administer as an IV infusion.

Supplied in a single-dose vial as a 40 mg/mL injection solution; must dilute prior to administration.

Do not shake vial.

Administer via infusion pump using an in-line aseptic 0.2 or 0.22 micron filter.

Do not co-administer other medications through the same IV line.

Dilution

Withdraw required volume of toripalimab-tpzi and inject slowly into 100 mL or 250 mL infusion bag containing 0.9% sodium chloride injection; final concentration should be 1-3 mg/mL.

Do not shake diluted solution; mix solution by gentle inversion.

Rate of Administration

Administer first infusion over 60 minutes. If no infusion-related reactions occur, may administer subsequent infusions over 30 minutes.

Dosage

Adults

Nasopharyngeal Carcinoma

IV

First-line treatment of metastatic or recurrent, locally advanced NPC:240 mg once every 3 weeks as an IV infusion until disease progression, unacceptable toxicity, or up to 24 months, in combination with cisplatin and gemcitabine.

Previously treated unresectable or metastatic NPC: 3 mg/kg as an IV infusion once every 2 weeks until disease progression or unacceptable toxicity.

Dosage Modification for Adverse Reactions

Dosage reductions not recommended.

In general, withhold therapy for severe (grade 3) immune-mediated adverse reactions. Permanently discontinue drug for life-threatening (grade 4) immune-mediated adverse reactions and recurrent severe (grade 3) immune-mediated reactions that require systemic immunosuppressive treatment, or if unable to reduce corticosteroid dose to ≤10 mg of prednisone equivalent per day within 12 weeks of steroid initiation.

Table 1 outlines dosage modifications for adverse reactions that require different management from these general guidelines.

Resume in patients with complete or partial resolution (grade 0 to 1) after corticosteroid taper. Permanently discontinue if no resolution within 12 weeks of steroid initiation or inability to reduce prednisone to ≤10 mg daily (or equivalent) within 12 weeks of initiating steroids.

Table 1. Recommended Dosage Modification for Toripalimab-tpzi Adverse Reactions1
Adverse Reaction	Dosage Modification Based on Severity
Pneumonitis	Grade 2: Withhold Grade 3 or 4: Permanently discontinue
Colitis	Grade 2 or 3: Withhold Grade 4: Permanently discontinue
Hepatitis with no tumor involvement of the liver	AST or ALT increases to >3 and ≤8 times ULN OR total bilirubin increases to >1.5 and ≤3 times ULN: Withhold AST or ALT increases to >8 times ULN OR total bilirubin increases to >3 times ULN: Permanently discontinue
Hepatitis with tumor involvement of the liver	If baseline AST and ALT are ≤ULN at baseline in patients with liver involvement, withhold or permanently discontinue based on recommendations for hepatitis with no liver involvement Baseline AST or ALT is >1 and ≤3 times ULN and increases to >5 and ≤10 times ULN OR baseline AST or ALT is >3 and ≤5 times ULN and increases to >8 and ≤10 times ULN: Withhold Baseline AST or ALT is >ULN and increases to >10 times ULN OR total bilirubin increases to >3 times ULN: Permanently discontinue
Endocrinopathies	Grade 3 or 4: Withhold until clinically stable or permanently discontinue depending on severity
Nephritis with renal dysfunction	Grade 2 or 3 increased blood creatinine: Withhold Grade 4 increased blood creatinine: Permanently discontinue
Exfoliative dermatologic conditions	Suspected SJS, TEN, or DRESS: Withhold Confirmed SJS, TEN, or DRESS: Permanently discontinue
Myocarditis	Grade 2, 3, or 4: Permanently discontinue
Neurological toxicities	Grade 2: Withhold Grade 3 or 4: Permanently discontinue
Infusion-related reactions	Grade 1 or 2: Interrupt or slow the rate of infusion Grade 3 or 4: Stop infusion and permanently discontinue

Special Populations

Hepatic Impairment

No special population dosage recommendations at this time.

Renal Impairment

No special population dosage recommendations at this time.

Geriatric Patients

No special population dosage recommendations at this time.

Cautions for Toripalimab

Contraindications

None.

Warnings/Precautions

Severe and Fatal Immune-mediated Adverse Reactions

Severe and fatal immune-mediated adverse reactions may occur in any organ system or tissue. Reactions may occur at any time, generally during treatment but may also occur after drug is discontinued. Early identification and management needed to ensure safe use.

Monitor patients closely for symptoms and signs that may be clinical manifestations of underlying immune-mediated adverse reactions. Assess liver enzymes, creatinine, and thyroid function at baseline and periodically during treatment.

If suspected immune-mediated reactions occur, initiate appropriate workup to exclude alternative causes (including infection). Medically manage immune-mediated adverse reactions promptly; refer for specialty consultation as appropriate.

Withhold or permanently discontinue depending on nature and severity of reaction.

If treatment interruption or discontinuation required, administer systemic corticosteroids (1–2 mg/kg per day prednisone or equivalent) until improvement to grade ≤1; upon improvement, initiate corticosteroid taper and continue to taper over ≥1 month. Consider administration of other systemic immunosuppressants if reaction not controlled with corticosteroid therapy.

Pneumonitis

Immune-mediated pneumonitis reported.

In patients treated with other PD-1/PD-L1 blocking monoclonal antibodies, incidence of pneumonitis higher in patients with history of prior thoracic radiation.

Colitis

Immune-mediated colitis reported.

Cytomegalovirus infection/reactivation reported in patients with corticosteroid-refractory immune-mediated colitis. In patients with corticosteroid-refractory colitis, consider repeating infectious workup to exclude alternative etiologies.

Hepatotoxicity and Hepatitis

Immune-mediated hepatitis reported.

Adrenal Insufficiency

Primary and secondary adrenal insufficiency reported.

If grade 2 or higher adrenal insufficiency occurs, initiate symptomatic treatment, including hormone replacement therapy as clinically indicated. Withhold or permanently discontinue depending on severity.

Hypophysitis

Immune-mediated hypophysitis reported; may present with acute symptoms associated with mass effect (e.g., headache, photophobia, visual field cuts). May lead to hypopituitarism. If hypophysitis occurs, initiate hormone replacement therapy as clinically indicated. Withhold or permanently discontinue depending on severity.

Thyroid Disorders

Immune-mediated thyroid disorders reported. Thyroiditis may present with or without endocrinopathy. Hypothyroidism may follow hyperthyroidism. Initiate hormone replacement therapy or medical management of hyperthyroidism as clinically indicated. Withhold or permanently discontinue based on severity.

Type 1 Diabetes Mellitus

Type 1 diabetes mellitus reported.

Monitor patients for hyperglycemia or other signs and symptoms of diabetes. Initiate insulin therapy as clinically indicated. Withhold depending on severity.

Nephritis with Renal Dysfunction

Immune-mediated nephritis reported.

Dermatologic Adverse Reactions

Immune-mediated rash and dermatitis reported. Bullous and exfoliative dermatitis, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS), has occurred with anti-PD-1/PD-L1 monoclonal antibodies.

For treatment of mild to moderate non-exfoliative rashes, topical emollients and/or topical corticosteroids may be adequate. Withhold or permanently discontinue depending on severity.

Other Immune-mediated Adverse Reactions

Other important immune-mediated adverse reactions reported; in some instances, reactions were severe or fatal.

Specific reactions have included cardiac/vascular disorders (myocarditis, pericarditis, vasculitis); neurologic disorders (meningitis, encephalitis, myelitis and demyelination, myasthenic syndrome/myasthenia gravis [including exacerbation], Guillain-Barré syndrome, nerve paresis, autoimmune neuropathy); ocular disorders (uveitis, iritis, other ocular inflammatory toxicities); GI disorders (pancreatitis, gastritis, duodenitis); musculoskeletal disorders (myositis/polymyositis, rhabdomyolysis and associated sequelae, arthritis, polymyalgia rheumatica, dermatomyositis); hypoparathyroidism; and other hematologic/immune disorders (hemolytic anemia, aplastic anemia, hemophagocytic lymphohistiocytosis, systemic inflammatory response syndrome, histiocytic necrotizing lymphadenitis [Kikuchi lymphadenitis], sarcoidosis, immune thrombocytopenic purpura, solid organ transplant rejection, other transplant [including corneal graft] rejection).

Some cases of ocular adverse reactions may be associated with retinal detachment. Various grades of visual impairment (including blindness) can occur. If uveitis occurs in combination with other immune-mediated adverse reactions, consider a Vogt-Koyanagi-Harada–like syndrome.

Infusion-related Reactions

Severe or life-threatening infusion-related reactions, including hypersensitivity and anaphylaxis, reported.

Monitor for signs and symptoms (e.g., rigors, chills, wheezing, pruritus, flushing, rash, hypotension, hypoxemia, and fever). For mild (grade 1) or moderate (grade 2) infusion-related reactions, interrupt or slow rate of infusion. For severe (grade 3) or life threatening (grade 4) infusion-related reactions, stop infusion and permanently discontinue.

Complications of Allogeneic Hematopoietic Stem Cell Transplantation

Serious or fatal complications can occur in patients who receive allogeneic hematopoietic stem cell transplantation (HSCT) before or after treatment with anti-PD-1/PD-L1 antibodies. Complications include hyperacute graft-versus-host disease (GVHD), acute GVHD, chronic GVHD, hepatic veno-occlusive disease after reduced intensity conditioning, and steroid-requiring febrile syndrome without an identified infectious cause.

Closely monitor patients for evidence of transplant-related complications and intervene promptly. Weigh benefits versus risks of therapy prior to or after allogeneic HSCT.

Embryo-fetal Toxicity

May cause fetal harm based on its mechanism of action and animal studies.

Perform pregnancy testing in females of reproductive potential prior to initiating toripalimab-tpzi. Advise pregnant women of the potential risk to fetus. Advise females of reproductive potential to use effective contraception during treatment with toripalimab-tpzi and for 4 months after last dose.

Immunogenicity

Treatment-emergent anti-drug antibodies (ADA) reported. Due to low incidence of ADA, effects of antibodies on safety, efficacy, pharmacokinetics, and/or pharmacodynamics are unknown.

Specific Populations

Pregnancy

May cause fetal harm based on its mechanism of action and animal reproductive studies. No available human data. Inhibition of PD-1/PD-L1 pathway has been shown to increase risk of immune-mediated rejection of developing fetus, resulting in death. Since human IgG₄is known to cross the placenta, toripalimab-tpzi has potential to be transmitted from mother to developing fetus. Advise pregnant women of potential risk to a fetus.

Lactation

Unknown whether toripalimab-tpzi is distributed into human milk, or if drug has any effects on breastfed infant or on milk production. Maternal IgG known to be distributed into human milk. Effects of local GI exposure and limited systemic exposure to toripalimab-tpzi in breast-fed infant are unknown.

Advise women to not breast-feed during treatment and for 4 months after last dose.

Females and Males of Reproductive Potential

Perform pregnancy testing in females of reproductive potential prior to treatment initiation. Advise females of reproductive potential to use effective contraception during treatment and for 4 months after last dose.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Studies did not include sufficient numbers of patients ≥65 years of age to determine whether pharmacokinetics are affected by age. No overall differences in safety were observed between elderly and younger patients.

Hepatic Impairment

No clinically significant differences in pharmacokinetics observed in patients with mild hepatic impairment. Pharmacokinetics not studied in patients with moderate or severe hepatic impairment.

Renal Impairment

No clinically significant differences in pharmacokinetics observed in patients with mild renal impairment. Pharmacokinetics not studied in patients with moderate or severe renal impairment.

Common Adverse Effects

Most common adverse reactions (≥20%) with toripalimab-tpzi in combination with cisplatin and gemcitabine: nausea, vomiting, decreased appetite, constipation, hypothyroidism, rash, pyrexia, diarrhea, peripheral neuropathy, cough, musculoskeletal pain, upper respiratory infection, insomnia, dizziness, malaise.

Most common adverse reactions (≥20%) with toripalimab-tpzi as single agent: fatigue, hypothyroidism, musculoskeletal pain.

Drug Interactions

No formal drug interaction studies to date.

Toripalimab Pharmacokinetics

Absorption

Bioavailability

Concentrations increased non-linearly over dose range of 0.3-10 mg/kg every 2 weeks.

Steady state reached by week 7.

Elimination

Metabolism

Metabolized into small peptides by catabolic pathways.

Half-life

10 ± 1.5 days after first dose and 18 ± 9.4 days at steady state.

Stability

Storage

Parenteral

Solution for Injection

Store unopened vials at 2-8°C in original carton to protect from light; do not freeze.

Prior to use, store diluted IV solution in refrigerator at 2-8°C for up to 24 hours or in room temperature at 20-25°C for up to 8 hours, from the time of dilution to completion of the infusion. Discard solution if not used within 8 hours if stored at room temperature or 24 hours if stored in refrigerator. If diluted solution is refrigerated, allow solution to come to room temperature prior to administration.

Actions

IgG₄ kappa immunoglobulin that is selective for PD-1, an immune-checkpoint receptor expressed on activated T-cells, monocytes, B-cells, natural killer (NK) T-cells, and dendritic cells.
Overexpression of PD-1 ligands on surface of tumor cells results in activation of PD-1 activity and suppression of cytotoxic T-cell activity.
Toripalimab blocks interaction between PD-1 and its ligands, resulting in enhanced immune response, including enhanced antitumor immune response.

Advice to Patients

Advise the patient to read the FDA-approved patient labeling (Medication Guide).
Inform patients of the risk of immune-mediated adverse reactions that may be severe or fatal, may occur after discontinuation of treatment, and may require corticosteroid treatment and interruption or discontinuation of toripalimab. These reactions may include pneumonitis, colitis, hepatitis, endocrinopathies, nephritis, severe skin reactions, or other immune-mediated adverse reactions.
Advise patients to contact their healthcare provider immediately for new or worsening cough, chest pain, or shortness of breath.
Advise patients to contact their healthcare provider immediately for diarrhea or severe abdominal pain.
Advise patients to contact their healthcare provider immediately for jaundice, severe nausea or vomiting, or easy bruising or bleeding.
Advise patients to contact their healthcare provider immediately for signs or symptoms of adrenal insufficiency, hypophysitis, hypothyroidism, hyperthyroidism, or Type 1 diabetes mellitus.
Advise patients to contact their healthcare provider immediately for signs or symptoms of nephritis.
Advise patients to contact their healthcare provider immediately for any signs or symptoms of severe skin reactions.
Advise patients that other immune-mediated adverse reactions can occur and may involve any organ system. Advise patients to contact their healthcare provider immediately for any new or worsening signs or symptoms.
Advise patients of the risk of solid organ transplant rejection and to contact their healthcare provider immediately for signs or symptoms of organ transplant rejection.
Advise patients to contact their healthcare provider immediately for signs or symptoms of infusion-related reactions.
Advise patients of the risk of post-allogeneic hematopoietic stem cell transplantation complications.
Advise patients of the importance of keeping scheduled appointments for blood work or other laboratory tests.
Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.
Advise patients that toripalimab can cause harm to a fetus and to inform their healthcare provider of a known, suspected, or planned pregnancy. Advise females of reproductive potential to use effective contraception during treatment with toripalimab and for 4 months after the last dose.
Advise patients not to breastfeed during treatment with toripalimab and for 4 months after the last dose.
Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care. For further information on the handling of antineoplastic agents, see the ASHP Guidelines on Handling Hazardous Drugs at [Web].

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.