Telisotuzumab vedotin: Drug information

For additional information see "Telisotuzumab vedotin: Patient drug information"

For abbreviations, symbols, and age group definitions show table

Brand Names: US

Emrelis

Pharmacologic Category

Antineoplastic Agent, Antibody Drug Conjugate;
Antineoplastic Agent, Antimicrotubular;
Antineoplastic Agent, MET Inhibitor;
Antineoplastic Agent, Monoclonal Antibody

Dosing: Adult

Dosage guidance:

Safety: For patients who experience an infusion-related reaction, administer premedications (per below table) prior to subsequent infusions.

**Recommended** **Premedications for Subsequent Doses for Patients Who Experience Telisotuzumab Vedotin Infusion-Related Reactions**
Medication, dose, and route	Dosing window (prior to telisotuzumab vedotin infusion)
H₁ antihistamine: Diphenhydramine 25 to 50 mg IV or Oral (or equivalent)	Administer 30 to 60 minutes prior to each telisotuzumab vedotin infusion
H₂ antihistamine: Famotidine 20 mg IV or Oral (or equivalent)	Administer 30 to 60 minutes prior to each telisotuzumab vedotin infusion
Antipyretic: Acetaminophen 650 to 1,000 mg IV or Oral (or equivalent)	Administer 30 to 60 minutes prior to each telisotuzumab vedotin infusion
Glucocorticoid: Methylprednisolone 125 mg IV (or equivalent) (or equivalent)	Administer 30 to 60 minutes prior to each telisotuzumab vedotin infusion

Clinical considerations: Select patients for treatment based on the presence of high c-Met protein expression (≥50% of tumor cells with strong [3+] staining).

Non–small cell lung cancer, nonsquamous, locally advanced or metastatic, c-MET protein overexpressing

Non–small cell lung cancer, nonsquamous, locally advanced or metastatic, c-MET protein overexpressing (≥50% of tumor cells with strong [3+] staining): IV: 1.9 mg/kg (maximum dose: 190 mg [in patients weighing ≥100 kg]) once every 2 weeks; continue until disease progression or unacceptable toxicity (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Note: Kidney function estimated using the Cockcroft-Gault formula.

CrCl 30 to 89 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling; however, there were no clinically significant differences in pharmacokinetics of the antibody drug conjugate or unconjugated monomethyl auristatin E observed with mild or moderate kidney impairment.

CrCl <30 ml/minute: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

End-stage kidney disease (with or without dialysis): There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Dosing: Liver Impairment: Adult

Mild impairment (total bilirubin ≤ ULN and AST > ULN or total bilirubin >1 to ≤1.5 times ULN and any AST): No dosage adjustment necessary.

Moderate or severe impairment (total bilirubin >1.5 times ULN and any AST): Avoid telisotuzumab vedotin use.

Dosing: Obesity: Adult

Note: Per the manufacturer’s labeling, the maximum dose for patients ≥100 kg is 190 mg.

American Society of Clinical Oncology guidelines for appropriate systemic therapy dosing in adults with cancer with a BMI ≥30 kg/m²: The dosing in the FDA-approved prescribing information should be followed in all patients, regardless of obesity status. If a patient with a BMI ≥30 kg/m² experiences high-grade toxicity from systemic anticancer therapy, the same dosage modification recommendations should be followed for all patients, regardless of obesity status (Ref).

Dosing: Adjustment for Toxicity: Adult

**Telisotuzumab Vedotin Recommended Dosage Reduction Levels**
Dose level	Recommended telisotuzumab vedotin dose and schedule
Usual (initial) dose	1.9 mg/kg (maximum dose: 190 mg) once every 2 weeks
First dosage reduction	1.6 mg/kg (maximum dose: 160 mg) once every 2 weeks
Second dosage reduction	1.3 mg/kg (maximum dose: 130 mg) once every 2 weeks
Third dosage reduction	1 mg/kg (maximum dose: 100 mg) once every 2 weeks
Permanently discontinue telisotuzumab vedotin in patients unable to tolerate 1 mg/kg once every 2 weeks.

**Telisotuzumab Vedotin Recommended Dosage Modifications for Adverse Reactions**
Adverse reaction	Severity	Telisotuzumab Vedotin Dosage Modification
^a ILD = Interstitial lung disease.
Edema, peripheral	≥ Grade 2	First occurrence: Withhold telisotuzumab vedotin until recovery to ≤ grade 1, then resume at the same dose. Subsequent occurrence: Withhold telisotuzumab vedotin until recovery to ≤ grade 1, then resume at the next lower dose level.
Infusion-related reaction	Grades 1 to 3	Interrupt telisotuzumab vedotin infusion and provide supportive treatment. Resume infusion with a 50% reduction of the infusion rate. For subsequent doses, increase the infusion rate as tolerated. Administer premedications prior to all future doses for patients who experienced infusion reactions.
Infusion-related reaction	Grade 4	Permanently discontinue telisotuzumab vedotin. Administer supportive treatment.
Neurologic toxicity: Peripheral neuropathy	Grade 2 or 3	Withhold telisotuzumab vedotin until recovery to ≤ grade 1, then resume at the next lower dose level.
Neurologic toxicity: Peripheral neuropathy	Grade 4	Permanently discontinue telisotuzumab vedotin.
Ocular toxicity: Keratitis	Grade 2	Withhold telisotuzumab vedotin. Refer patient to eye care professional for ophthalmic exam and treatment (eg, lubricating and/or steroid eye drops). Resume telisotuzumab vedotin at the same dose at the discretion of the healthcare provider.
Ocular toxicity: Keratitis	Grade 3 or 4	Refer patient to eye care professional for ophthalmic exam and treatment (eg, lubricating and/or steroid eye drops). Permanently discontinue telisotuzumab vedotin.
Pulmonary toxicity: ILD^a/pneumonitis	Grade 1	Withhold telisotuzumab vedotin and consider corticosteroids as soon as ILD^a/pneumonitis is suspected. Resume telisotuzumab vedotin upon radiographic resolution.
Pulmonary toxicity: ILD^a/pneumonitis	≥ Grade 2	Permanently discontinue telisotuzumab vedotin.
Other adverse reactions	Grade 3	First occurrence: Withhold telisotuzumab vedotin until recovery to ≤ grade 1, then resume at the same dose. Subsequent occurrence: Withhold telisotuzumab vedotin until recovery to ≤ grade 1, then resume at the next lower dose level.
Other adverse reactions	Grade 4	Permanently discontinue telisotuzumab vedotin.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.

>10%:

Cardiovascular: Peripheral edema (22%)

Endocrine & metabolic: Decreased serum albumin (61%), decreased serum calcium (47%), decreased serum glucose (11%), decreased serum magnesium (14%), decreased serum phosphate (33%), decreased serum potassium (14%), decreased serum sodium (30%), increased serum glucose (58%)

Gastrointestinal: Constipation (14%), decreased appetite (22%), nausea (15%)

Hematologic & oncologic: Decreased hemoglobin (35%; grades 3/4: 4%), decreased platelet count (14%; grades 3/4: <1%), decreased white blood cell count (16%; grades 3/4: 1%), lymphocytopenia (37%; grades 3/4: 10%)

Hepatic: Increased gamma-glutamyl transferase (36%), increased serum alanine aminotransferase (41%), increased serum alkaline phosphatase (30%), increased serum aspartate aminotransferase (34%)

Nervous system: Fatigue (29%), peripheral neuropathy (51%; grades 3/4: 11%; peripheral sensory neuropathy [45%], peripheral motor neuropathy [9%])

Ophthalmic: Ophthalmic signs and symptoms (ocular surface disorders: 25%; including blurred vision [15%; including decreased visual acuity], dry eye syndrome [5%], keratitis [11%; including corneal cyst, corneal edema, corneal erosion, corneal opacity, punctate keratitis])

Renal: Increased serum creatinine (16%)

Respiratory: Pneumonia (13%)

1% to 10%:

Endocrine & metabolic: Hypermagnesemia (10%)

Gastrointestinal: Vomiting (10%; grades 3/4: <1%)

Hematologic & oncologic: Decreased neutrophils (10%; grades 3/4: 1%)

Hypersensitivity: Infusion-related reaction (3%)

Nervous system: Dizziness (<10%)

Neuromuscular & skeletal: Arthralgia (<10%)

Ophthalmic: Photophobia (<10%)

Respiratory: Interstitial lung disease (≤10%), pleural effusion (2%), pneumonitis (≤10%)

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Infusion-related reactions: Telisotuzumab vedotin may cause infusion-related reactions (IRRs). Signs/symptoms of IRRs include dyspnea, flushing, chills, nausea, chest discomfort, and hypotension. The median time to onset of IRR was 28 days (range: 1 to 43 days). In the clinical study, IRRs occurred in a small percentage of patients who received telisotuzumab vedotin; rare grade 3 and 4 IRRs were reported, some leading to permanent discontinuation.

• Ocular toxicity: Telisotuzumab vedotin can cause ocular surface disorders, including blurred vision, visual impairment, keratitis, and dry eye. In the clinical study, ocular surface disorders occurred in one-fourth of telisotuzumab vedotin–treated patients. The most common ocular surface disorders were blurred vision, keratitis, and dry eye; grade 3 ocular surface disorders (blurred vision and keratitis) occurred in a small number of patients. The median time to onset of ocular surface disorders was 47 days (range: 1 to 319 days).

• Peripheral neuropathy: Telisotuzumab vedotin may cause peripheral neuropathy (including peripheral sensory neuropathy and peripheral motor neuropathy). In the clinical study, peripheral neuropathy occurred in approximately one-half of patients treated with telisotuzumab vedotin; including grade 3 events. These adverse reactions included peripheral sensory neuropathy in almost half of patients and peripheral motor neuropathy in a small percentage of patients. The median time to onset of peripheral neuropathy was 105 days (range: 1 to 472 days). Peripheral neuropathy led to permanent discontinuation of telisotuzumab vedotin some patients. The median time to onset of peripheral neuropathy leading to treatment discontinuation was 249 days (range: 57 to 519 days). A small number of patients had ongoing motor neuropathy as of the last telisotuzumab vedotin dose; with most experiencing persistent grade 1 or 2 symptoms 30 days after the last dose. Signs/symptoms of new or worsening peripheral neuropathy include hypoesthesia, hyperesthesia, paresthesia, a burning sensation, neuropathic pain, and/or muscle weakness.

• Pulmonary toxicity: Telisotuzumab vedotin may can cause severe, life-threatening, or fatal interstitial lung disease (ILD)/pneumonitis. In the clinical study, ILD/pneumonitis was reported with telisotuzumab vedotin, including grade 3 or 4 events and cases of fatal ILD/pneumonitis. The median time to onset of ILD/pneumonitis was 48 days (range: 23 to 85 days). ILD/pneumonitis led to permanent discontinuation in a small percentage of patients; the median time to onset of ILD/pneumonitis leading to treatment discontinuation was 46 days (range: 23 to 85 days). Advise patients to immediately report cough, dyspnea, fever, and/or any new or worsening respiratory symptoms.

Dosage form specific issues:

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Ref). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Ref). See manufacturer’s labeling.

Other warnings/precautions:

• Appropriate use: Select patients for treatment of nonsquamous non–small cell lung cancer based on the presence of high c-MET protein overexpression (≥50% of tumor cells with strong [3+] staining), as determined by an approved test. Information on tests approved for detection of high c-MET protein overexpression is available at http://www.FDA.gov/CompanionDiagnostics.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous [preservative free]:

Emrelis: Telisotuzumab vedotin-tllv 20 mg (1 ea); Telisotuzumab vedotin-tllv 100 mg (1 ea) [contains polysorbate 80]

Generic Equivalent Available: US

Pricing: US

Solution (reconstituted) (Emrelis Intravenous)

20 mg (per each): $3,355.20

100 mg (per each): $16,776.00

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Prescribing and Access Restrictions

Telisotuzumab vedotin is available through specialty distributors. Examples from the manufacturer can be found at https://www.emrelishcp.com/support#howtoorderemrelis.

Administration: Adult

IV: Infuse over 30 minutes via a dedicated infusion line with a 0.2- or 0.22-micron in-line filter made of polyethersulfone, polyvinylidene fluoride, or polyamide. If refrigerated, allow solution to reach room temperature prior to administration. Do not infuse other medications through the same infusion line.

Monitor for signs/symptoms of infusion reactions during infusion. If an infusion reaction occurs, withhold, reduce the rate of infusion, or permanently discontinue telisotuzumab vedotin based on severity.

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2024) list; however, it meets the criteria for a hazardous drug. Telisotuzumab vedotin contains manufacturer’s special handling information (MSHI) and is a hazardous drug (per the product labeling). Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (Ref).

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:

Emrelis (telisotuzumab vedotin-tllv): https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/761384s000lbl.pdf#page=19

Use: Labeled Indications

Non–small cell lung cancer, nonsquamous, locally-advanced or metastatic, c-MET protein overexpressing: Treatment of locally advanced or metastatic, nonsquamous non–small cell lung cancer (NSCLC) in adults with high c-MET protein overexpression (≥50% of tumor cells with strong [3+] staining), as determined by an approved test, who have received a prior systemic therapy.

Medication Safety Issues

Sound-alike/look-alike issues:

Telisotuzumab vedotin may be confused with atezolizumab, brentuximab vedotin, enfortumab vedotin, polatuzumab vedotin, tafasitamab, tarlatamab, teclistamab, telotristat ethyl, tislelizumab, tisotumab vedotin, teplizumab, tezepelumab, tocilizumab, toripalimab, tremelimumab.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of CYP3A4 (Major), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor

CYP3A4 Inducers (Strong): May decrease serum concentration of Telisotuzumab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be decreased. Risk C: Monitor

CYP3A4 Inhibitors (Strong): May increase serum concentration of Telisotuzumab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. Risk C: Monitor

Efgartigimod Alfa: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Nipocalimab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Rozanolixizumab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Reproductive Considerations

Verify pregnancy status prior to initiating treatment in patients who could become pregnant.

Patients who could become pregnant should use effective contraception during therapy and for 2 months after the last dose of telisotuzumab vedotin. Patients with partners who could become pregnant should also use effective contraception during therapy and for 4 months after the last telisotuzumab vedotin dose.

Adverse effects to fertility were observed in animal toxicology studies; data are lacking on possible fertility effects in humans.

Pregnancy Considerations

Telisotuzumab vedotin is a humanized monoclonal antibody (IgG_1k) conjugated to monomethyl auristatin E (MMAE). Based on the mechanism of action and data from animals administered MMAE, in utero exposure to telisotuzumab vedotin may cause fetal harm.

Breastfeeding Considerations

It is not known if telisotuzumab vedotin is present in human milk.

Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 1 month after the last telisotuzumab vedotin dose.

Monitoring Parameters

Monitor CBC with differential and liver function tests (at baseline and periodically during treatment). Verify pregnancy status prior to initiating treatment in patients who could become pregnant. Monitor for ocular surface disorders during treatment. Monitor for signs/symptoms of new or worsening peripheral neuropathy (eg, hypoesthesia, hyperesthesia, paresthesia, a burning sensation, neuropathic pain, muscle weakness) and ILD/pneumonitis. Monitor during infusion for signs/symptoms of infusion reactions.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (Ref) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow up.

Mechanism of Action

Telisotuzumab vedotin is a c-MET–directed antibody drug conjugate (ADC) composed of a humanized immunoglobulin G1 kappa (IgG1κ) monoclonal antibody conjugated to the small molecule microtubule-disrupting agent monomethyl auristatin E (MMAE) via a cleavable dipeptide linker (Ref). Following binding to c-MET (the cell surface receptor for hepatocyte growth factor) on expressing cells, telisotuzumab vedotin undergoes internalization and intracellular cleavage of MMAE, disrupting the microtubule network of actively dividing cells, and inducing cell cycle arrest and apoptosis. Telisotuzumab vedotin demonstrated antitumor activity NSCLC animal models.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: V_d: Telisotuzumab vedotin: 3.4 L.

Protein binding: Monomethyl auristatin E (MMAE): 68% to 82%.

Metabolism: Telisotuzumab vedotin is expected to undergo catabolism to small peptides, amino acids, and unconjugated MMAE and unconjugated MMAE-related catabolites; MMAE is primarily metabolized via CYP3A4.

Half-life elimination: Antibody drug conjugate (ADC): ~3 days; MMAE: ~4 days.

Time to peak: ADC: At end of infusion; MMAE: ~5 days after infusion.

Excretion: Clearance: ADC: 1.3 L/day; MMAE: 76 L/day.

Alade SL, Brown RE, Paquet A Jr. Polysorbate 80 and E-Ferol toxicity. Pediatrics. 1986;77(4):593-597. [PubMed 3960626]
Camidge DR, Bar J, Horinouchi H, et al. Telisotuzumab vedotin monotherapy in patients with previously treated c-Met protein-overexpressing advanced nonsquamous EGFR-wildtype non-small cell lung cancer in the phase II LUMINOSITY trial. J Clin Oncol. 2024;42(25):3000-3011. doi:10.1200/JCO.24.00720 [PubMed 38843488]
Centers for Disease Control (CDC). Unusual syndrome with fatalities among premature infants: association with a new intravenous vitamin E product. MMWR Morb Mortal Wkly Rep. 1984;33(14):198-199. [PubMed 6423951]
Emrelis (telisotuzumab vedotin) [prescribing information]. North Chicago, IL: AbbVie Inc; May 2025.
Griggs JJ, Bohlke K, Balaban EP, et al. Appropriate systemic therapy dosing for obese adult patients with cancer: ASCO guideline update. J Clin Oncol. 2021;39(18):2037-2048. doi:10.1200/JCO.21.00471 [PubMed 33939491]
Hodson L, Ovesen J, Couch J, et al; US Centers for Disease Control and Prevention, National Institute for Occupational Safety and Health. Managing hazardous drug exposures: information for healthcare settings, 2023. https://doi.org/10.26616/NIOSHPUB2023130. Updated April 2023. Accessed December 27, 2024.
Hwang JP, Feld JJ, Hammond SP, et al. Hepatitis B virus screening and management for patients with cancer prior to therapy: ASCO provisional clinical opinion update. J Clin Oncol. 2020;38(31):3698-3715. doi:10.1200/JCO.20.01757 [PubMed 32716741]
Isaksson M, Jansson L. Contact allergy to Tween 80 in an inhalation suspension. Contact Dermatitis. 2002;47:313. doi:10.1034/j.1600-0536.2002.4705104.x [PubMed 12534540]
Lucente P, Iorizzo M, Pazzaglia M. Contact sensitivity to Tween 80 in a child. Contact Dermatitis. 2000;43(3):172. [PubMed 10985636]
Ovesen JL, Sammons D, Connor TH, et al; US Centers for Disease Control and Prevention, National Institute for Occupational Safety and Health. NIOSH list of hazardous drugs in healthcare settings, 2024. https://doi.org/10.26616/NIOSHPUB2025103. Updated December 18, 2024. Accessed December 20, 2024.
Refer to manufacturer's labeling.
Shelley WB, Talanin N, Shelley ED. Polysorbate 80 hypersensitivity. Lancet. 1995;345(8980):1312-1313. doi:10.1016/s0140-6736(95)90963-x [PubMed 7746084]
United States Pharmacopeia. <800> Hazardous Drugs—Handling in Healthcare Settings. In: USP-NF. United States Pharmacopeia; July 1, 2020. Accessed January 16, 2025. doi:10.31003/USPNF_M7808_07_01

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Telisotuzumab vedotin: Drug information

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