Phase I-trial of a methotrexate — Albumin conjugate (MTX-HSA) in cancer patients
G. HartungG. StehleH. SinnH. H. SchrenkS. HeegerM. KränzleH.H. FiebigW. Maier‐BorstD. L. HeeneW. Queißer
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IAA-conjugate formation in carrot tissues transformed with aux- Ti plasmids was induced by exogenously applied IAA. When the tissues were treated with NAA or 2, 4-D, IAA-conjugate formation was also induced. This result suggests that IAA-conjugate formation may be generally induced by substances having auxin activity.On the other hand, 2, 4-D was not metabolized to conjugate form even when the transformed carrot tissues were treated with IAA. This suggests that the effect of 2, 4-D is different from that of IAA in carrot.
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Daucus carota
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Abstract Benzalcyanoacetamides were designed and synthesized as reversible thiol conjugate addition acceptors. These thia‐conjugate additions can rapidly and reversibly achieve equilibrium under aqueous conditions at neutral pH. Kinetic studies show that electron‐withdrawing groups at the 4‐position of the phenyl ring of the benzalcyanoacetamides promote the conjugate addition at equilibrium. Dynamic thiol exchange of these conjugate acceptors is faster than singly activated α,β‐unsaturated carbonyl compounds. These thia‐conjugate additions can be assembled as potentially useful components in dynamic combinatorial chemistry.
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Thiol
Aqueous medium
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To the Editor.—
In answer to Dr. Auerbach's letter concerning maintenance dosage of methotrexate, I certainly agree that methotrexate should not be maintained when conventional therapy will control the psoriasis. In our article, we pointed out that methotrexate was to be used only in severe cases of psoriasis which were unresponsive to conventional methods of therapy. Certainly, I would agree that methotrexate should be withdrawn as quickly as possible, but clinically this is often impossible. Many patients with severe psoriasis will flare in two to three weeks if their methotrexate is suddenly stopped. We have even seen some cases of rebound with more severe psoriasis as is seen after oral corticosteroid therapy. Our approach has been to maintain the patient on methotrexate 25 mg/week, orally, until their psoriasis is cleared. We then will gradually reduce this dose of methotrexate and attempt to withdraw the drug especially during the summer monthsClearance
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Fifty five patients of extensive psoriasis were treated with oral weekly methotrexate. All patients responded promptly to methotrexate therapy. Relapse was observed after variable periods following stoppage of methotrexate. Safety, efficacy, maintenance dose, relapse and long term effects of methotrexate in psorasis are discussed.
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Conjugate beam method
Phase conjugation
Complex conjugate
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저자들은 융모성질환의 화학치료에 있어서 methotrexate 치료도중 문제가 될 수 있는 약제의 독성을 줄이고, 내성을 방지하기 위하여 leucovorin rescue를 주는 적절한 시기 및 용량을 결정하고자 methotrexate 포화검사를 시행하여 다음과 같은 결론을 얻었다. 1. Methotrexate혈중치는 methotrexate의 정맥내 주사후 30분에 최고 농도에 달하며, 그 반감기는 5.04±2.05 시간이었다. 2. Methotrexate정맥내 주사후 24시간후와 28시간후에 30mg이 folic acid를 줄때 혈중 methotrexate 평균농도는 24시간후에 50μmole/liter였고, 48시간후에 0.32μmole/liter이었다. 3. Methotrexate치료중 약제의 독성과 반감기를 비교해 본 결과 반감기가 평균보다 긴 경우 그 약제의 독성이 강한 것으로 보이나 통계적인 유효성은 없는 것으로 나타났다. Methotrexate 치료중 약제의 족성과 methotrexate 정맥주사후 48시간의 methotrexate 혈중치를 비교해 본 결과 간독성에 있어서는 유의한 차이가 없으나, 혈액학적 독성에 있어서는 methotrexate 혈중치가 평균보다 높은군이 낮은군에 비해 강한 독성이 나타났다. 이상과 같이 저자들은 methotrexate의 항암화학 요법에 있어서 강한 약제의 독성을 나타낼 가능성이 있는 환자를 알아내는데에 methotrexate 포화검사가 유용하게 쓰일 수 있으며, 약제의 독성을 나타낼 가능성이 큰 환자에 있어서는 methotrexate 혈중농도를 측정하여야 그에 따른 leucovorin rescue를 시행하여야 한다고 결론지었다.
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A modified procedure has been worked out for preparing a conjugate of porcine insulin with E. coli beta-galactosidase employing a heterobifunctional reagent, N-hydroxysuccinimidyl m-maleimidobenzoate. Optimal conditions for insulin acylation and subsequent coupling with beta-galactosidase were selected that afforded the conjugate in a high yield. The ability of the modified antigen to react with antibody was evaluated in the reaction of conjugate binding with immobilized monoclonal antibody to insulin. The conjugate almost completely retained the enzymatic activity and reacted with high specificity with the antibody to insulin. The conjugate can be used in competitive ELISA of insulin.
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Objective To investigate the effect of mifepristone in combination with methotrexate for the medical treatment of ectopic pregnancy. Methods All patients with ectopic pregnancy for medical management were analysed retrospectively.Treatment consisted of methotrexate injected intramuscularly and 400 mg of mifepristone, administered orally,compared with a previous group who received only methotrexate alone.Results Success rate was 85% in combination group. Success rate was similar with that in methotrexate alone group.The time until Serum (3- hCG resolution in combination group was(22.64±6.77)d versus(27.22±6.11)d in methotrexate alone group( P 0.05). Conclusion The success rate of mifepristone in combination with methotrexate was similar to that of methotrexate alone. The time until Serum (3 - hCG resolution in combination group was shorter than that in methotrexate alone group.
Medical treatment
Abortifacient
Combination therapy
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[reaction: see text] The first examples of conjugate additions of N-tert-butanesulfinyl metalloenamines are reported. Highly stereoselective conjugate additions (97:3 to 99:1 dr) were observed between metalloenamines derived from N-sulfinyl ketimines and alpha,beta-unsaturated ketones bearing either alkyl or aryl substituents. The conjugate addition products could rapidly be converted with high diastereoselectivity to 2,4,6-trisubstituted piperidines, which are difficult to access by other methods.
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