ADC TOXICITY ATLAS
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Vobramitamab duocarmazine

Discontinued
MGC018; MGC-018; vobra duo; AEX4089DC1; anti-B7-H3 ADC
Sponsor
MacroGenics
Indication
Metastatic castration-resistant prostate cancer (mCRPC)
Target family
Immunoglobulin superfamily
RP2D dose
2.7 mg/kg
Q4W (every 4 weeks)RP2D
01
Multi-organ toxicity

Fingerprint & organ drill-down

Also reported
0%severity100%
0
Assessed · clear
true 0%
No data
never assessed
4 adverse-event terms

Ocular

Any-grade
19.8%
G3+
-
RP2D
sagittal schematic · -

Tissues shaded by reported adverse-event rate.

Cornea
AE
-
Express.
-
Limbus
AE
-
Express.
-
Conjunctiva
AE
19.8%
Express.
-
Lens
AE
-
Express.
-
Retina / RPE
AE
-
Express.
-
Dominant tissue
Conjunctiva
Surface subtype
Mixed
Reversibility
-
Reported ocular events
Conjunctivitis12.2%
Dry eye11.1%
Eyelid oedema6.7%
Lacrimation increased5.6%
02
Construct

Molecular anatomy

Antibody
IgG1
Humanized
Linker
Cleavable
2.7
DAR
Payload
DNA minor-groove alkylator (cell-cycle independent)
Linker structureC36H54N8O14
CC(C)C(NC(=O)OCCOCCN1C(=O)C=CC1=O)C(=O)NC(CCCNC(N)=N)C(=O)Nc1ccc(COC(=O)N(C)CCN(CCOCCO)C(=O)O)cc1
Payload structureC29H23ClN4O4
CC1=C2C(=CC=C1)C(=CC3=C2[C@@H](CN3C(=O)C4=CN5C=C(C=CC5=N4)NC(=O)C6=CC=C(C=C6)O)CCl)O
03
Antibody

Antibody & Fc engineering

Antibody
Vobramitamab
Isotype
IgG1
Origin
Humanized
Fc modifications
None
Glycoengineering
Standard
Effector silencing
None
FcγR binding
Retained
C1q binding
Retained
04
Linker & conjugation

Linker chemistry

Linker profile
Linker
vc-seco-DUBA (Mal-PEG2-Val-Cit-PABA-cyclization spacer)
Class
Cleavable
Cleavage
Cleavable
Attachment
Cysteine (interchain)
Conjugation
Interchain cysteine (maleimide)
Symmetry
Symmetric
DAR (mean)
2.7
DAR homogeneity
Heterogeneous
Plasma t½
-
Cleavage trigger
Cathepsin B (Val-Cit)
Release control
Conditional
Hydrophilicity mask
Discrete-PEG-spacer
Formula
C36H54N8O14
Linker MW
822.87 Da
Linker TPSA
297.8 Ų
Linker xLogP
-0.1919
ADCdb linker
LIN0HGTZQ
In-vitro stability
-
05
Payload

Payload & physicochemistry

Payload profile
Payload
seco-DUBA (duocarmazine)
Class
Duocarmycin
Mechanism
DNA minor-groove alkylator (cell-cycle independent)
Released catabolite
DUBA (activated duocarmycin)
Mechanistic subtype
DNA-alkylator
Stereochem / salt
Unknown
Bystander
Yes
PAMPA rank
-
MW
527 Da
XLogP3
5.3
logD₇.₄
3.7
TPSA
107 Ų
pKa
6.0 pKa
Charge pH 7.4
0
H-bond donors
3
H-bond acceptors
5
IC50 (HCEC)
-
Formula
C29H23ClN4O4
PubChem CID
46240929
ADCdb payload
PAY0SOSMQ
Hydrophobicity · logD₇.₄
hydrophilic −2+3.7+4 lipophilic
Bioactivity note
Free payload seco-DUBA in vitro cytotoxicity IC50 (ADCdb cell-line data): A375.S2 181 pM; Calu-6 260 pM; PA-1 275 pM; Hs 700T 319 pM; NCI-H1703 585 pM; MDA-MB-468 767 pM; LN-229 910 pM; SW48 1447 pM; Raji >10 nM. Mechanism: DNA minor-groove alkylator (seco-CBI duocarmycin warhead
06
Dosing & regimen

Dosing

RP2D dose
2.7 mg/kg
Schedule
Q4W (every 4 weeks)
Route
IV
Fractionated
No
n at RP2D
86
Dose basis
TBW
Trial phase
Phase 2
Dose-OAE available
Yes
Tox summary basis
RP2D
07
Ocular & expression

Ocular profile & eye-tissue target expression

Target profile
OAE any-grade
19.8 %
OAE grade 3+
-
OAE data status
reported
Severity (weighted)
-
Keratopathy
-
Conjunctival
19.8 %
Dry eye
11.6 %
Blurred vision
-
Dominant tissue
Conjunctiva
Surface subtype
Mixed
Grading scale
CTCAE v5
Reversibility
-
Target expression in eye tissues (HCA detection · HPA bulk)
Cornea (central)
-
Cornea (limbal)
-
Conjunctiva
-
RPE
-
Retina (HPA)
-
Cross-trial comparability · source-verified
Ascertainment: Systematic eye examsScale: CTCAE v5Denominator: RP2D
08
Identity & registry

Identifiers, registry & notes

ADC id
vobramitamab-duocarmazine
Approval status
Discontinued
Approval year
-
UniProt
Q5ZPR3
ADCdb ADC
DRG0DEGEG
ADCdb antibody
ANI0EIMTT
ADCdb target
TAR0RIOXT
Primary source
ClinicalTrials.gov NCT05551117 (TAMARACK) posted results; ESMO 2024 abstract 1654P (Ann Oncol 2024); Shenderov ESMO 2021 Ph1 poster 620P (NCT03729596); ADCdb DRG0DEGEG/LIN0HGTZQ
Aliases & development codes
MGC018; MGC-018; vobra duo; AEX4089DC1; anti-B7-H3 ADC
Notes
ADC: Vobramitamab duocarmazine (MGC018 / vobra duo), MacroGenics anti-B7-H3 (CD276) humanized IgG1 ADC with a Byondis-derived vc-seco-DUBA duocarmycin (DNA-alkylating) payload, DAR ~2.7. Linker LIN0HGTZQ and payload seco-DUBA (PAY0SOSMQ) are SHARED with trastuzumab-duocarmazine (DRG0THGAW) already in the DB; linker SMILES/formula/MW/TPSA/xLogP and payload physchem are taken from that shared chemistry. CONJUGATION DISCREPANCY: ADCdb lists conjugation/site as "Random Lysines," which is inconsistent with the maleimide ("Mal-PEG2-Val-Cit-PABA") linker and the shared Byondis vc-seco-DUBA platform. A maleimide attaches to interchain cysteine thiols, so I report conjugation as interchain Cys (maleimide), matching trastuzumab-duocarmazine. Flag for reconciliation. RP2D / DOSE SELECTION: TAMARACK (NCT05551117) is a randomized Phase 2 dose-optimization in mCRPC testing 2.0 mg/kg Q4W (ITT n=91) vs 2.7 mg/kg Q4W (ITT n=90); CT.gov safety populations N=90 and N=86. 2.7 mg/kg gave higher confirmed ORR (41% vs 20%) and was the dose carried into the Part 2 expansion, so I designate RP2D = 2.7 mg/kg Q4W (primary cohort = Part 1 Arm B, N=86, line_context=RP2D); the 2.0 mg/kg arm is included as comparator rows. NOTE: the 2.0 mg/kg arm was clearly better tolerated (fewer effusions, PPE, cytopenias), and MacroGenics suggested mitigation via longer interval (e.g. Q6W) or loading dose. The Phase 1 (CP-MGC018-01, NCT03729596) RP2D was 3.0 mg/kg Q3W. The entire program was DISCONTINUED on 2024-07-23 (remaining n=32 stopped) and TAMARACK is TERMINATED, on the totality of efficacy + emerging safety. OCULAR (priority): Best source is the ClinicalTrials.gov posted results (final, MedDRA 27.1, >=5% threshold) - more complete than the paywalled ESMO 2024 poster 1654P. At RP2D (2.7 mg/kg): conjunctivitis 19.8% (17/86, the max ocular PT -> oae_any_pct=19.8), dry eye 11.6%, eyelid oedema 10.5%, lacrimation increased 5.8%; at 2.0 mg/kg: conjunctivitis 12.2%, dry eye 11.1%, eyelid oedema 6.7%, lacrimation 5.6%. Keratitis, blurred vision and photophobia were each <5% (below threshold) despite being protocol-monitored AESIs with mandatory prophylactic eye drops (corticosteroid/antihistamine/artificial tears TID), no-contact-lens and lid-hygiene instructions, and dose hold/reduce/discontinue rules. Only 1 serious ocular event in the whole trial (1 serious dry eye, 2.0 mg/kg arm); ocular AEs were low-grade (ESMO 2024: AEs >=10% were mostly grade 1-2). ocular_surface_subtype set to "Mixed" (conjunctival + ocular-surface + eyelid, without corneal keratopathy or visual-acuity loss); this differs from the corneal-microcyst pattern of MMAF/maytansinoid ADCs. oae_g3plus_pct left blank (registry gives serious/non-serious, not CTCAE grade; no explicit G3+ ocular count published). NOTE the ocular signal is more apparent in TAMARACK Phase 2 than in the Phase 1 poster (where ocular AEs were not in the >=10% TRAE table, i.e. <10%). GRADE DATA CAVEAT: CT.gov posted results report AEs split into Serious vs Other(non-serious, >=5%) categories, NOT by CTCAE grade. All toxicity_rows therefore use grade_bucket="Any" with the non-serious >=5% incidence as the headline figure; material serious-AE counts are given in the row notes. Pleural effusion is reported at the ESMO 2024 any-grade values (44.2% at 2.7 mg/kg; 28.8% at 2.0 mg/kg; tier D) because the registry split (non-serious 33.7%/27.8% + serious 14.0%/7.8%) understates the true any-grade union. Overall Grade >=3 TEAE rate was >50% (ESMO 2024). HALLMARK TOXICITIES not in the organ_system enum: pericardial effusion (serosal; pooled TAMARACK 15.3%; 2.7 mg/kg non-serious 15.1% + serious 5.8%; 2.0 mg/kg 14.4% + 1.1%) and palmar-plantar erythrodysaesthesia (PPE) syndrome (2.7 mg/kg 27.9% (24/86); 2.0 mg/kg 21.1% (19/90); pooled 23.3%). Also prominent: asthenia (2.7 mg/kg 60.5%, 2.0 mg/kg 52.2%), peripheral oedema (40.7%/36.7%), decreased appetite (40.7%/36.7%), fatigue (23.3%/27.8%). Pericardial/pleural effusions were the doses-limiting serosal-toxicity theme that, with fatal pneumonitis, drove the program's discontinuation. Sources: ADCdb DRG0DEGEG and linker LIN0HGTZQ (idrblab.net); ClinicalTrials.gov NCT05551117 (TAMARACK) posted results (authoritative AE source); MacroGenics ESMO 2024 abstract 1654P via UroToday/MacroGenics coverage; Shenderov et al., ESMO 2021 poster 620P, MGC018 Phase 1 cohort expansion (NCT03729596); shared seco-DUBA/vc-seco-DUBA chemistry per trastuzumab-duocarmazine DB row.