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. 2025 Jul 19;167(1):196. doi: 10.1007/s00701-025-06612-6

Table 2.

Characteristics of studies on mIDH-inhibitors, n:7

Number of patients Main Findings in relation to mIDH-inhibitor administration
Study Design mIDH-inhibitor Median treatment duration (range) Total, n Tumor Grade (G), Previous therapy, n (%) Aim Survival QoL Toxicities Treatment Response/ORR (%)
Cho et al. (2022) [9] R

-Ivosidenib (AG-120)

-Vorasidenib (AG-881)

Follow-up:

Up to 4 months post-treatment

Ivosidenib: 18

Vorasidenib: 11

G2/3/4:

n:19/7/3

%: 66/24/10

NR To investigate MRI changes in gliomas during mIDH-inhibitor treatment at 3–6 weeks and/or 2–4 months after treatment start NA NR NR

Radiological observations:

At 3–6 weeks:

Increase in

nrCBV and median nrCBV/ADC but not in ADC or FLAIR

At 2–4 months: No changes from baseline

Mellinghoff et al. (2021) [32] P, Open-label Vorasidenib (AG-881) Enhancing: 3.3 months (0.2–53.6) Non-enhancing: 26.8 months (1.0–50.9)

Total Glioma: 52

Enhancing: 30

Non-enhancing: 22

G2/3/4:

n:25/22/4

%: 48/42/8

Unknown: n:1

%: 2

Enhancing:

-RT:

22 (73)

-Systemic:

25 (83)

-Only Surgery:

4 (13)

Non-enhancing:

-RT:

8 (36)

-Systemic:

14 (64)

-Only surgery:

7 (32)

Investigate safety and outcomes of Vorasidenib

Median PFS:

-Overall Cohort: 7.5 months

-Enhancing: 3.6 months

-Non-enhancing: 36.8 months

NR

Any CTCAE, n: 52,

most common:

Headache 46.2%

ALT elevation 44.2%

CTCAE ≥ 3, n:10 ALT/AST elevation, Fatigue, Nausea, Seizure, Vomiting, Decreased neutrophil count

Enhancing:

ORR (0.0)

Non-enhancing:

ORR (18.2)

Mellinghoff et al. (2023) [30] RCT, Open-label Ivosidenib (AG-120) Vorasidenib (AG-881)

Vorasidenib: 14.3 months (0.9 −22.6)

Ivosidenib:

15.1 months

(1.8–22.1)

Vorasidenib: 24 Ivosidenib: 25

Vorasidenib:

G2/3:

n: 22/2

%: 92/8

Ivosidenib:

G2/3:

n:21/4

%: 84/16

Vorasidenib:-Surgery:24 (100)-RT:7 (29)-Systemic:10 (42)Ivosidenib:-Surgery:25 (100)-RT: 7 (28)-Systemic: 14 (56) To investigate the mechanism of action of Vorasidenib and Ivosidenib Median PFS not reached in either mIDH-inhibitor NR

Vorasidenib:

-Any CTCAE, n: 24,

most common:

Nausea, Headache 41.7%,

Diarrhea, Fatigue 29.2%

-CTCAE ≥ 3, n:7

Anemia, ALT-elevation, hyperglycemia, hypophosphatemia

Ivosidenib:

-Any CTCAE, n:25,

most common:

Headache, Anemia 36.0%, Diarrhea, Seizure 28.0%

-CTCAE ≥ 3, n:6, hyponatremia

Vorasidenib

−50mg q.d.:

ORR (42.9)

−10mg q.d.:

ORR (10.0)

Ivosidenib

−500 mg q.d.:

ORR (35.7)

−250 mg b.i.d.:

ORR (12.5)

2-HG concentration reduction:

-Vorasidenib 50 mg q.d.: 92.6% reduction

-Ivosidenib 500 mg q.d.: 91.1% reduction

Mellinghoff et al. (2023) [31] RCT, Double-blinded Vorasidenib (AG-881)

Median follow-up (Interquartile range):

Vorasidenib: 14.0 months

(10.1 to 17.9)

Placebo:

14.3 months (10.0 to 18.1)

Vorasidenib: 168

Placebo: 163

G2:

n:331

%: 100

Surgery: 331 (100) Investigate PFS and time to next intervention in grade 2 tumors receiving Vorasidenib

Vorasidenib vs

placebo:

-PFS:

27.7 vs. 11.1 months

-Time to next intervention:

not reached vs. 17.8 months

NR

-Any CTCAE, n:141, most common: ALT elevation 38.9%, Fatigue 32.3%

-CTCAE ≥ 3, n:27, ALT/AST/gamma-glutamyl transferase elevation, Fatigue, Diarrhea, Seizure

Vorasidenib

40 mg q.d.:

ORR (10.7)

Placebo: ORR (2.5)

Natsume et al. (2022) [39] P, Open-label Safusidenib (DS-1001)

Enhancing:

7.3 weeks

(0.0–190.0)

Non-enhancing

91.2 weeks

(15.0–207.0)

Total: 47

Enhancing: 35

Non-enhancing: 12

G2/3/4

n:17/23/7

%36/49/15

RT:47 (100)Chemotherapy:38 (81)-TMZ:35 (75)-Nimusutine14 (30)-Bevacizumab 7 (15)

To determine the safety, efficacy and pharmacology of Safusidenib/

DS-1001

Median PFS Non-enhancing vs. Enhancing:

not reached vs.10.4 weeks

NR

-All CTCAE, n:45,

most common:

Skin hyperpigmentation 53.2%

Diarrhea 46.8%

-CTCAE 3, n: 20, Diarrhea, Arthralgia, headache, decreased neutrophil count, ALT/AST elevation

-Significantly lower

2-HG in Safusidenib (DS-1001) tumor samples

-Enhancing:

ORR (17.1)

(CR: n: 2, 5.7%,

PR: n: 4, 11.4%)

-Non-enhancing:

ORR (33.3) (PR: n: 1, 8.3%, mR: n: 3, 25.0%)

Peters et al. (2023) [43] R Ivosidenib (AG-120) 43.7 weeks (5.5- 74.1)

Total: 30

Enhancing: 8

Non-enhancing: 22

G2/3/4:

n:21/8/1

%:70/27/3

RT: 8 (27)TMZ: 18(60)mIDH-peptide vaccine: 2 (7)Bevacizumab1 (3) To investigate the outcomes of Ivosidenib treatment Deaths: n:2 (of total 30) NR

CTCAE 1, n:23,

most common:

Diarrhea 26.7%,

Elevated creatine kinase 33.3%

Enhancing:

ORR (0.0)

Non-enhancing:

ORR (36.3)

Wick et al. (2021) [65] P BAY1436032 NR

Total glioma:39

Enhancing: 33

Non-enhancing: 2

Unknown: 4

Dose expansion glioma: 25

Dose escalation glioma: 14

NR Dose expansion: -RT: 23 (92)Dose escalation:NR separately To investigate the safety profile and pharmacology of BAY1436032 in mIDH solid tumors PFS rate at 3 months: 0.31 NR NA due to analysis with other tumor types ORR: (11) (CR: n:1, 3.0%, PR: n:3, 9.0%)

2-HG; 2-hydroxyglutarate, ADC; Apparent diffusion coefficient, ALT; alanine aminotransferase, AST; aspartate aminotransferase, b.i.d.; bis in die, twice a day, CR; Complete Response, CTCAE; Common terminology criteria for adverse events, FLAIR; Fluid-attenuated inversion recovery, G; Tumor grade, mIDH; mutant-isocitrate dehydrogenase, mR; minor Response, MRI; Magnetic Resonance Imaging, NA; Not Applicable, NR; Not reported, nrCBV; normalized relative cerebral blood volume, ORR; Objective response rate, P; Prospective, PFS; Progression Free Survival, PR; Partial Response, q.d.; quaque die, once a day, QoL; Quality of Life, R; Retrospective, RCT; Randomized controlled trial, RT; Radiotherapy, TMZ; Temozolomide, vs.; versus