LEUKEMIA: CHRONIC MYELOGENOUS

 

Regimen/Number

Of Patients

Drug Dose and Route

Leukopenia/

Neutropenia

Toxicity

Anemia

Toxicity

Other

Grade III-IV Toxicities

Emetogenic

Potential

Consequences of

Adverse Event(s)

  CML:Hydroxyurea

(Hehlmann R, et al.

Blood.

1994;84:4064-77)

 

N = 194

 

CML:Hydroxyurea 40 mg/kg/d PO

 

 

Cytopenias*

Mild Nausea*

Dermatologic*

Drug Fever*

 

*common toxicity,

frequency not reported

Daily―

level 1

Treatment discontinued

due to toxicity in < 1%

of patients

CML:Interferon

(Guilhot F, et al.

N Engl J Med.

1997;337:223-29)

 

N = 361

CML:Interferon 5 MU/m2 SQ daily

 

Note: Decrease dose by 50% for granulocyte

count < 1500/mm3 and/or platelets<100000/mm3

Hematologic

toxicity (other)

2.5%

 

Nausea/vomiting/

Diarrhea 3.8%

Mucositis 1%

Other GI 1%

Weight Loss/Asthenia 5.5%

Skin Rash 2%

Fever, Flu-like

syndrome 2%

Peripheral Neuropathy 1%

Central Neurologic

Syndrome 1%

Depression 5.8%

Other Psychologic 5.3%

Cytolytic Hepatic 1%

Other Toxicity 8.8%

Thrombocytopenia 2.2%

Level 1

97 patients discontinued

therapy due to toxicity

42 deaths―mostly

related to allogeneic

or autologous BMT or

disease progression

Interferon

Cytarabine

(Guilhot F, et al.

N Engl J Med.

1997;337:223-29)

 

N = 360

 

Interferon 5 MU/m2 SQ daily

Cytarabine 20 mg/m2/d SQ days 1-10 every month

 

Note:

Decrease dose by 50% for granulocyte

count < 1500/mm3 and/or platelets

< 100,000/mm3.

Cytarabine held for WBC < 3000/mm3 and

platelets < 100,000/mm3; cytarabine

discontinued for granulocyte count

< 1000/mm3 and platelets < 50,000/mm3.

If hematologic control is not achieved, then

increase cytarabine to 40 mg/m2/d SQ days 1-15.

Hematologic

toxicity (other)

8.6%

 

 

Nausea/Vomiting/

Diarrhea 12.5%

Mucositis 5.8%

Other GI 1%

Weight Loss/

Asthenia 13.3%

Skin Rash 5.2%

Fever, Flu-like

Syndrome 3%

Depression 4.2%

other psychologic 3.6%

Cytologic Hepatitis 2.5%

Other Toxicity 8.6%

Thrombocytopenia 5.5%

Level 1

94 patiwnts discontinued

therapy due to toxicity

deaths―monstly

related to allogeneic

or autologous BMT or

disease progression

 

 

LEUKEMIA: CHRONIC MYELOGENOUS (continued ) : Page 2

 

Regimen/Number

Of Patients

Drug Dose and Route

Leukopenia/

Neutropenia

Toxicity

Anemia

Toxicity

Other

Grade III-IV Toxicities

Emetogenic

Potential

Consequences of

Adverse Event(s)

STI-571/Imatinib

mesylate

(kantarjian H, et al.

N Engl J Med.

2002;346:645-52)

 

N = 532

Chronic Phase

Imatinib mesylate 400 mg orally daily

 

Note: The dose was increased to 400 mg

orally twice daily in those in whom a

complete hematologic response was not

achieved after 3 month of treatment;

in those whose disease relapsed within

3 month after the achievement of a

complete hematologic response; and

in those in whom a major cytogenetic

response had not been achieved after

12 months of therapy.

Neutropenia

Grade III 27%

Grade IV 8.1%

Leukopenia

Grade III 22%

Grade IV 1.7%

Grade III 6%

Grade IV 1.1%

Febrile

Neutropenia 0.75%*

Thrombocytopenia 20%

Muscle cramps 0.9%

Rash and Related Events 3%

Nausea 1.5%

Vomiting 0.6%

Diarrhea 0.9%

Superficial Edema 1.1%

Weight Gain 4.3%

Arthralgia 0.8%

Fatigue 0.4%

*Grade unknown,

classified as

serious drug-related

adverse event

Level 2

Median time to first

Grade III or Grade IV

episode of neutropenia

was 62 days

Drug-related adverse

events led to treatment

discontinuation in

11 (2.1%) patients

STI-571/Imatinib

mesylate

(Sawyers CL, et al.

Blood.

2002;99:3530-39)

 

N = 260

Blast crisis

Imarinib 400 mg or 600 mg orally daily

(administered once a day with a meal)

 

Note: Starting dose increased to 600 mg

orally daily after first 37 patients; dose

was permitted to be Increased to a

maximum of 400 mg orally twice daily in

patients who relapsed, and in patients who

did not achieve a hematologic response

after at least 1 month of treatment.

Neutropenia

Grade III

(400 mg)

14%

Grade III

( 600 mg)

16%

Grade IV

(400 mg)

54%

Grade IV

(600 mg)

47%

Grade III

(400 mg)

43%

Grade III

(600 mg)

40%

Grade IV

(400 mg)

16%

Grade IV

(600 mg)

10%

Thrombocytopenia 62%

Hyperbilirubinemia

(Grade III) 4%

Transaminases:

AST (Grade III) 2%

ALT (Grade III) 2%

Nausea 2%

Vomiting 1%

Diarrhea 0.8%

Hemorrhage 2.3%

Musuloskeletal pain < 1%

Muscle Cramps < 1%

Dermatitis/Rash 4%

Fluid-Retention Events 6%

Superficial

Edema 3.5%

Other Fluid-Retention

Events 3.1%

Level 3

Development of

cytopenias dependent

on stage of disease.

with a frequency of

Grade III-IV neutro-

penia between 2 and

3 times higher in blast

crisis and accelerated

phase compared with

chronic phase

Hematologic side

effects managed

with a dose reduction

or interruption (see

prescribing information

for recommendations)

adverse events led to a

temporary or perma-

nent reduction in the

initial dose of imatinib

on one or more occa-

sions in 46% of

patients started on

400 mg daily and in

47% of patients started

on 600 mg daily

Drug-related adverse

events leading to

discontinuation to

occurred in 5% of

patients (all on 600 mg dose)

 

 

LEUKEMIA: CHRONIC MYELOGENOUS (continued ) : Page 3

 

Regimen/Number

Of Patients

Drug Dose and Route

Leukopenia/

Neutropenia

Toxicity

Anemia

Toxicity

Other

Grade III-IV Toxicities

Emetogenic

Potential

Consequences of

Adverse Event(s)

STI-571/Imatinib

mesylate

(Talpaz M, et al. Blood.

2002;99:1928-37)

 

N = 235

(400 mg = 77;

600 mg = 158)

Accelerated Phase

Imatinib 400 mg or 600 mg orally daily (administered once a day with a meal)

 

Note: Starting dose increased after first

77 patients; dose was able to be escalated

to 400 mg orally twice daily in patients who

had a relapse, or in those patients who did

not achieve a hematologic response after

at least 1 month of treatment.

 

Neutropenia

Grade III

(400 mg)

21%

Grade III

(600 mg)

25%

Grade IV

(400 mg)

35%

Grade IV

(600 mg)

35%

Leukopenia

Grade III

(400 mg)

27%

Grade III

(600 mg)

35%

Grade IV

(400 mg)

18%

Grade IV

(600 mg)

13%

Grade III

(400mg) 35%

Grade III

(600 mg) 32%

Grade IV

(400 mg) 9%

Grade IV

(600 mg) 15%

Thrombocytopenia 43%

Nausea 3%

Vomiting 1%

Fluid Retention 1 %

Edema 3%

Diarrhea 0.4%

Hemorrhage 2%

Transaminases (Grade III)

AST 2%

ALT 3%

Hyperbilirubinemia

(Grade III) 2%

Dermatitis 1%

Fatigue 3%

Arthralgia 3%

 

Level 3

Development of

cytopenias dependent

on stage of disease,

with a frequency of

Grade III-IV neutropenia

between 2 and 3 times

higher in blast crisis

and accelerated phase

compared with chronic

phase

Hematologic side effects

managed with a dose

reduction or interruption

(see prescribing

information for

recommendations)

Adverse events led

to dose reduction in

49% of patients on

400 mg and 52% on

600 mg dose

Adverse events leading

to treatment

discontinuation

occurred in 2.5 % of

patients (all in the

600 mg orally

daily group )

1 death suspected to

be related to toxicity

(liver failure)