2. Emiltatug ledadotin

Emiltatug ledadotin (Emi-Le; XMT-1660) is a B7-H4-targeted antibody-drug conjugate (ADC). Emiltatug ledadotin consists of the tumor-specific anti-B7-H4 monoclonal antibody Emiltatug (HY-P990918) and the linker-payload system Ledadotin (HY-177541), with site-specific conjugation achieved via GlycoConnect click chemistry. Emiltatug ledadotin inhibits the growth of B7-H4-positive cancer cells. Emiltatug ledadotin can be used to study advanced solid tumors with B7-H4 overexpression, particularly breast cancer, ovarian cancer, and endometrial cancer.

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Emiltatug ledadotin

Emiltatug ledadotin Chemical Structure

CAS No. : 2855974-40-0

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Emiltatug ledadotin Related Antibodies

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Description

Emiltatug ledadotin (Emi-Le; XMT-1660) is a B7-H4-targeted antibody-drug conjugate (ADC). Emiltatug ledadotin consists of the tumor-specific anti-B7-H4 monoclonal antibody Emiltatug (HY-P990918) and the linker-payload system Ledadotin (HY-177541), with site-specific conjugation achieved via GlycoConnect click chemistry. Emiltatug ledadotin inhibits the growth of B7-H4-positive cancer cells. Emiltatug ledadotin can be used to study advanced solid tumors with B7-H4 overexpression, particularly breast cancer, ovarian cancer, and endometrial cancer[1][2].

In Vitro

Emiltatug ledadotin (3 days) potently induces target-dependent cytotoxicity in HEK293-B7-H4 cells, with a payload-based IC50 of 1 nM[2].
Emiltatug ledadotin (3 days) potently induces cytotoxicity in CAMA-1 breast cancer cells, with a payload-based IC50 of 0.052 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Emiltatug ledadotin Related Antibodies
Parmacokinetics
Species Dose Route T1/2 CL Vdss Bioavailability Cmax AUC
Rat[1] 10 mg/kg p.o. / / / 33.1 % 2.4 μg/mL 14.2 μg·h/mL
Rat[1] 2 mg/kg i.v. 1.7 h 4.0 mL/min/kg 0.5 L/kg / / /
Dog[1] 5 mg/kg p.o. / / / 57.6 % 4.8 μg/mL 11.9 μg·h/mL
Dog[1] 2 mg/kg i.v. 2.1 h 4.1 mL/min/kg 0.5 L/kg / / /
In Vivo

Emiltatug ledadotin (1.5/0.05-4.7/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the HBCx-24 breast cancer PDX model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (2.3/0.075-4.7/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the MX-1 breast cancer CDX model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (2.3/0.075-4.6/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the OV2423 ovarian cancer PDX model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (4.6/0.15 mg/kg; i.v.; single dose) induces potent tumor growth inhibition in the CTG-1692 ovarian cancer PDX model following a single intravenous dose of 4.6/0.15 mg/kg (antibody/payload)[2].
Emiltatug ledadotin (1.5/0.05-4.6/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the PD-1 refractory mBR9013 syngeneic breast cancer model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (4.7/0.15 mg/kg; i.v.; single dose) exhibits antitumor activity in 43% of a diverse panel of breast cancer PDX models following a single intravenous dose of 4.7/0.15 mg/kg (antibody/payload), with activity correlating with B7-H4 expression[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HSD: Athymic Nude-Foxn1mu (female)[2]
Dosage: 1.5/0.05 mg/kg; 2.3/0.075 mg/kg; 4.7/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Induced complete tumor regression at all tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 63 post-treatment at the 4.7/0.15 mg/kg dose.
Animal Model: Crl:NU(Ncr)-Foxn1mu (female)[2]
Dosage: 2.3/0.075 mg/kg; 4.7/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 63 post-treatment at the 4.7/0.15 mg/kg dose.
Animal Model: BALB/cNj-Foxn1nu/Gpt (female)[2]
Dosage: 2.3/0.075 mg/kg; 4.6/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 70 post-treatment at the 4.6/0.15 mg/kg dose.
Animal Model: HSD: Athymic Nude-Foxn1mu (female)[2]
Dosage: 4.6/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Induced significant tumor growth inhibition, with mean tumor volume remaining near baseline through day 56 post-treatment, while vehicle-treated tumors grew to over 2000 mm3.
Animal Model: FVB/NJ (female; PD-1 refractory model)[2]
Dosage: 1.5/0.05 mg/kg; 4.6/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 49 post-treatment at the 4.6/0.15 mg/kg dose.
Showed no antitumor activity with anti-PD-1 treatment.
Animal Model: HSD: Athymic Nude-Foxn1mu (female)[2]
Dosage: 4.7/0.15 mg/kg (antibody/payload)
Administration: i.v.; single dose
Result: Achieved median best response (MBR) ≤ -0.3 (≥ 30% tumor shrinkage) in 12/28 (43%) models.
Saw tumor volume reduction in 13/28 (46%) models.
Had more frequent responses in TNBC models (9/15, 60%) than ER-positive models (3/13, 23%).
Showed activity correlating with B7-H4 expression, with 9/13 (69%) models with high tumor proportion score (TPS ≥ 75) achieving MBR ≤ -0.3.
CAS No.
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[Emiltatug ledadotin]
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Emiltatug ledadotin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Emiltatug ledadotin2855974-40-0Emi-Le XMT-1660XMT1660XMT 1660XMT-1660auristatin F-HPAmicrotubulesHEK293-B7-H4 cellssyngeneic breast cancer modelsB7-H4breast cancertriple-negative breast cancerovarian cancerovarian cancer xenograft modelsxenograft breast cancer modelsInhibitorinhibitorinhibit

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